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65 results about "Liver microsomes" patented technology
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Human Liver Microsomes. Human liver microsomes contain a wide variety of drug metabolizing enzymes and are commonly used to support in vitro ADME (Absorption, Distribution, Metabolism and Excretion) studies. These microsomes are used to examine the potential for first-pass metabolism of orally administered drugs.
Cultivation method of Cyp gene knocked-out rats, and preparation method of liver microsome of the rats
ActiveCN106148416ADiverse in vitro modelsImprove transfer abilityMicroinjection basedFermentationHepaticaMicro injection
The invention provides a cultivation method of Cyp gene knocked-out rats, and a preparation method of liver microsome of the rats. The Cyp gene knock-out herein includes Cyp single gene knock-out and Cyp multiple gene knock-out. In the method, firstly a Cyp gene knocked-out rat is constructed by means of a CRISPR / Cas system, which includes selection of a knocked-out target site, in-vitro synthesis and transcription of sg RNA and Cas9m RNA, preparation of a pseudopregnant female rat, in-vitro micro-injection and transplanting of a single-cell embryo, and cultivation of the rat, and finally, a homozygote Cyp gene knocked-out rat can be cultured. Furthermore, the liver of the Cyp gene knocked-out rat is extracted and is subjected to homogenization and differential centrifugation to prepare the liver microsome of the rat in Cyp gene deletion. The invention also provides an application of the Cyp gene knocked-out rats and the liver microsome thereof in study on drug metabolism.
Owner:EAST CHINA NORMAL UNIV
Oxadiazole-contained cyclic compound, preparation method, intermediates, compositions and application thereof
ActiveCN107954999AStrong inhibitory activityImprove bioavailabilityGroup 4/14 element organic compoundsSenses disorderMetaboliteCancer cell
The invention discloses an oxadiazole-contained cyclic compound, a preparation method, intermediates, compositions and application thereof. The medically acceptable salts, the enantiomer, the diastereoisomer, the tautomer, the solvate, the metabolite or the prodrug of the dthe oxadiazole-contained cyclic compound shown as the formula I is high in inhibitory activity on IDO (dioxygenase) at a molecular level and a cellular level and significant in proliferation inhibition effects on cancer cells related to IDO activity at an animal level and good in liver microsome stability of human, mouse andthe like, has no significant inhibition over metabolic enzymes and achieves good absorption properties and high bioavailability in rats and mice as well as good druggability.
Owner:SHANGAI PHARMA GRP CO LTD
Detection method for simultaneously determining metabolic products of seven CYP450 enzyme probe substrates in human liver microsomes
InactiveCN104849371AThe pretreatment method is simpleSuitable for routine testingComponent separationMetaboliteHepatica
The invention relates to a detection method for simultaneously determining the metabolic products of seven CYP450 enzyme probe substrate in human liver microsomes, and belongs to the technical field of biological detection. The detection method comprises the following steps: performing incubation on specificity probe substrates of CYP450 enzyme and the human liver microsomes for different periods of reaction time to generate corresponding metabolic products, using Zaltoprofen as an interior label, adopting a high performance liquid chromatography-tandem mass spectrometry after protein precipitation pretreatment, and thus simultaneously detecting the concentrations of the metabolic products of seven probe substrates. The method disclosed by the invention is high in specificity, high in sensitivity and simple and convenient in operation, and has already successfully been applied to the research of baicalin on CYP450 enzyme inhibiting action of the human liver microsomes.
Owner:WUXI PEOPLES HOSPITAL
Plant drug for treatment of liver disease
The present invention related to safe plant drug for treatment of liver disease, specifically, this invention proves a safe plant drug Schisandrin and its preparation. Schisandrin has the following pharmaceutical functions: increasing tumor suppresson genes express activity, decreasing activity of oncogenes, increasing immune function, increasing liver DNA synthesis, decreasing serum alamine aminotransferase activity, increasing glutathione level, increasing glutathione reductase activity, decreasing lipid peroxidation of liver, increasing hepatic microsomal monooxygenases activity, increasing ATP content in liver, increasing energy metabolism activity, decreasing density lipoprotein oxidation, protecting gastrointestinal function, increasing killer cell activity, increasing complement activity, decreasing induced liver cancer activity and decreasing grown of cancer cells.
Owner:ZHAO XINXIAN
Preparation method, detection method and application of probe drug composition for determination of metabolic activity of cytochrome P450
InactiveCN102650620AHigh sensitivityStrong specificityComponent separationIn-vivo testing preparationsDrugs solutionMicroparticle
The invention relates to a preparation method, a detection method and application of a probe drug composition for determination of metabolic activity of cytochrome P450. The composition mainly comprises a preparation made with a specific probe with major isoforms of CYP450, i.e. CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, as an active component. Cocktail probe drug solution is prepared, the probe drug composition is injected into an animal or liver microsomes for in vitro co-incubation, and the concentration of each probe drug is determined to assess the metabolic activity of the CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. In the early stage of research and development of new drugs, the effects of the drugs on the activity of each isoform of the cytochrome P450 are screened in a high-throughput way, and the interactions of the drugs can be predicted. In the stage of clinical research, the testing can be performed with the probe drug composition in an in-vivo probe method, and the effects of the drugs on the in-vivo metabolic activity of different isoforms of the human liver CYP450 can be examined.
Owner:TIANJIN MEDICAL UNIV
LC-MC method used for determining NNK metabolites in liver microsomes
ActiveCN102445510A: Simple pre-processingFast analysisComponent separationMaterial analysis by electric/magnetic meansNitrosoMetabolite
The invention relates to an LC-MC method used for determining NNK metabolites in liver microsomes and specifically to an LC-MC method used for analyzing and determining 4-(methyl nitroso)-1-(3-pyridyl)-1-butanone (NNK) metabolites in liver microsomes, which belongs to the field of biochemical analysis. The method provided in the invention mainly comprises the following steps: (1) preparation of an incubation system for liver microsomes; (2) sample treatment; (3) sample analysis and determination of NNK metabolites in the liver microsomes by using the LC-MC method. The invention has the following advantages of simple pre-treatment, a fast analysis speed, good selectivity, high detection sensitivity and capacity of analyzing and comparing the metabolism of NNK in different kinds of liver microsomes, can lay a methodological foundation for further research on in-vivo and in-vitro metabolism of NNK and other nitrosamine compounds and has critical significance.
Owner:ZHENGZHOU TOBACCO RES INST OF CNTC
Modified spectrophotometry for detecting activity of HMG-CoA reducase and applications thereof
InactiveCN102221531AWith bulk filteringThe conclusion is credibleMicrobiological testing/measurementColor/spectral properties measurementsFiltrationSystem optimization
The invention discloses a modified spectrophotometry for detecting activity of HMG-CoA reducase and applications thereof. The detecting method comprises the following steps: a. preparing liver microsome by centrifuging fresh liver organics; b. carrying out weight drop, homogenate, dilution and centrifugation on the liver microsome, then obtaining a supernatant, and obtaining the reducase source containing dissolvable HMG-CoA; c. detecting the protein content of HMG-CoA reducase source, and diluting the HMG-CoA reducase source to have the known concentration; and d. adding the HMG-CoA reducase source to the optimized reaction system, and detecting the OD340 value and calculating the enzyme activity. The detecting system for HMG-CoA reducase inhibitor is established on the basis of the detecting method and is used for calculating the enzyme activity inhibition rate and half-inhibition concentration (IC50), and can be used for screening hypolipidemic drugs. The modified spectrophotometry has the advantages of system optimization, high safety, low price, batch filtration, credible conclusion and the like, can effectively screen the HMG-CoA reducase activity inhibitor, and provides a simple and quick method for developing the hypolipidemic drugs.
Owner:WUHAN UNIV
Absolute quantitative method for biomass spectra of CYP450 enzyme hypotypes
The invention relates to an absolute quantitative method for biomass spectra of CYP450 enzyme hypotypes, and belongs to the technical field of proteomics. In the method, on the basis of liquid chromatography (LC) / mass spectrometry (MS) / MS, the absolute quantification of four CYP450 enzyme hypotypes, namely CYP1A2, CYP2B6, CYP3A4 and CYP3A5 in systems such as liver microsome and the like is realized simultaneously by a strategy that CYP450 generates specific peptide quantitative enzymes by pancreatic enzyme hydrolysis. The method mainly comprises the following steps of: preprocessing a proteinsample, preparing a standard curve, measuring the protein sample and preparing a quality control sample. The absolute quantitative method has excellent linear relations, is high in accuracy and repeatability, is sensitive, precise and reliable, and can be used for medicinal metabolism and the evaluation of the mutual effect of medicaments.
Owner:JILIN UNIV
Method for detecting inhibitory effect of drug on human liver cytochrome P450
InactiveCN102816830AAvoid and reduce interactionsMicrobiological testing/measurementDrug utilisationMetabolite
The invention provides a method for detecting the inhibitory effect of a drug on the human liver cytochrome P450. According to the invention, a probe drug, a to-be-detected drug and human liver microsomes containing the cytochrome P450 are subjected to incubation together, then metabolites of the probe drug are detected, and the inhibitory effect of the to-be-detected drug on the cytochrome P450 can be effectively detected; therefore, a convenient method for industrial drug research, development and screening and clinical medication guidance is provided.
Owner:SHANGHAI SIXTH PEOPLES HOSPITAL
2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and preparation method and application thereof
The invention provides 2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and a preparation method and application thereof. The derivative is 2, 3-bis(substituted phenyl)-5-subsituted arylmethyl-7-substituted benzylidene dihydro-pyrazolo piperidine derivative, having the following formula (I). The preparation method includes using substituted arylmethyl amine and methyl acrylate as raw materials; subjecting the materials to Michael addition, Dieckmann condensation and hydrolysis-decarboxylation sequentially; allowing for Aldol reaction with substituted benzaldehyde to obtain intermediate N-substituted arylmethyl-3, 5-bis(substituted benzylidene)-4-piperidone; allowing for condensation with substituted phenylhydrazine to obtain a compound according to the formula (I). The derivative is efficient in inhibiting multiplication of various carcinoma cell lines such as leukemia, esophagus cancer, ovarian cancer and breast cancer in human, is well stably metabolic in liver microsomes of human and rat, is free of direct and competitive inhibition on five enzymes of liver microsomes, such as CYP3A4, CYP2D6, CYP2C9, CYP1A2 and CYP2C19, is highly bioavailable, is low in toxicity to normal cells, and is available for the preparation of drugs for the cancers.
Owner:SHANGHAI NORMAL UNIVERSITY
Method for measuring paeoniflorin metabolic products in liver microsome
The invention discloses a method for measuring paeoniflorin metabolic products in liver microsome and belongs to the technical field of medical detection. The method provided by the invention mainly comprises the following steps: transforming paeoniflorin liver microsome; performing sample pretreatment; and measuring the paeoniflorin metabolic products in the liver microsome by a liquid chromatography-mass spectrometry combination method. The method has the advantages of simplicity and convenience in operation, simplicity in sample treatment, high analysis speed, high specificity and high sensitivity. The method can be used for detecting more metabolic products of the paeoniflorin in the liver microsome; furthermore, by adoption of the analysis method, the structure of the metabolic products can be speculated more and accurately, technical support is provided for researching in vitro metabolic products of the paeoniflorin in the liver microsome, and important significance in deep research on active products and the action mechanism thereof is achieved.
Owner:LIAONING UNIVERSITY
Liver microsome metabolism analysis of koumine and toxicokinetics of related animals
The invention discloses liver microsome metabolism analysis of koumine (KM) and toxicokinetics of related animals. The method disclosed by the invention mainly comprises the following steps: 1, performing KM liver microsome metabolism analysis comprising the following sub-steps: (1) establishing a KM incubation system; (2) performing sample treatment; and (3) performing sample analysis, namely selecting KM human related animals by comparing the liver microsome metabolism product distribution characteristics of KM in various experimental animals and the kinetic characteristics of various kinds of KM on KM metabolism; 2, performing KM macaca rhesus acute toxicity associated toxicokinetics comprising the following sub-steps: (1) performing blood sample collection and plasma sample treatment on infected experimental animals; (2) performing quantitative determination; and (3) performing blood concentration data analysis. The method has the advantages that due to the in-vitro liver microsome metabolism analysis of KM in various experimental animnals, the human related animals are selected for performing associated toxicokinetics study, so that the predictability of toxicity assessment of the experimental animals on clinical study is improved.
Owner:FUJIAN MEDICAL UNIV
Application of tetrahydropalmatine enantiomers in preparation of P-glycoprotein inhibitor
InactiveCN102100694AExpanded indicationsNo reversal effectOrganic active ingredientsAntineoplastic agentsMetabolic enzymesTumor chemotherapy
The invention provides application of tetrahydropalmatine enantiomers in preparation of P-glycoprotein inhibitor. The tetrahydropalmatine is one of main active ingredients of the Chinese herbal medicine rhizoma corydalis and comprises L-tetrahydropalmatine and D-tetrahydropalmatine. The research shows that the tetrahydropalmatine enantiomers can obviously inhibit the P-gp function, but the tetrahydropalmatine enantiomers are not the P-gp substrates; the tetrahydropalmatine enantiomers can obviously increase the concentration of anti-tumor medicine adriamycins in medicament-resistant tumor cells and reverse the multi-medicament resistance of tumor cells and do not have obvious effects of inhibiting and inducing main medicament metabolic enzymes of liver microsomes, so that the racemes, laevo isomers or dextro isomers of the tetrahydropalmatine enantiomers can be used as auxiliary medicaments for tumor chemotherapy, and the range of indications of the tetrahydropalmatine is expanded; and simultaneously, the invention provides the medicament for the assistant treatment for tumors, which alleviates pain, improves curative effect and is not addictive, for tumor patients.
Owner:ZHEJIANG UNIV
2,4-bis (trifluoroethoxy)pyridine compound and drug containing the compound
InactiveUS7223764B2Improved metabolic resistanceHigh concentrationOrganic active ingredientsOrganic chemistryHydrogen atomOral medication
The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1):(wherein X1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and to a drug containing the compound or the salt as an active ingredient.The compound has metabolic resistance in human liver microsome, good absorbability upon oral administration, and excellent ACAT inhibitory activity.
Owner:KOWA CO LTD
Novel medicine in-vitro incubation, metabolite searching, medicine-medicine interaction prediction quick screening and analysis integrated strategy
InactiveCN106770693AImprove research efficiencyShorten research timeComponent separationMetaboliteData acquisition
The invention discloses a method of quickly searching an in-vitro metabolite of a target compound and researching the subtype of a metabolic enzyme thereof by means of in-vitro human liver microsome incubation with combination of LC-Q-TOF / MS detection. The method is mainly used for researching of medicine-medicine interaction and mainly includes the steps of in-vitro incubating the target compound by the human liver microsomes, performing data collection and quick analysis to a sample by means of LC-Q-TOF / MS, and quickly searching the metabolites of the target compound and determining the subtype of the metabolic enzyme participating in the metabolism thereof. The method comprehensively considers the in-vitro human liver microsome incubation conditions and conditions of chromatography and mass spectrum data collection. In addition, with combination of related software for quickly analyzing the data, the metabolite of the target compound can be more accurately and quickly searched and found, and the subtype of the metabolic enzyme participating in the metabolism can be comprehensively determined, thus providing evidence for researching the medicine-medicine interaction.
Owner:CHINA PHARM UNIV
LC-MS/MS (liquid chromatography-tandem mass spectrometry) method for determining cordycepin metabolite in liver microsome
The invention belongs to the technical field of medicine detection, discloses an LC-MS / MS (liquid chromatography-tandem mass spectrometry) method for determining cordycepin metabolite in liver microsome, and particularly relates to the LC-MS / MS method for analyzing and determining the cordycepin metabolite in the liver microsome. The LC-MS / MS method mainly includes the steps of (1) incubation of the liver microsome containing cordycepin; (2) preprocessing of a sample; (3) analysis of the sample, thereby determining the cordycepin metabolite in the liver microsome. The LC-MS / MS has the advantages of convenience in operation, sample processing simplicity, high analysis speed, high specificity and high flexibility, provides technical support for researching extrametabolites of the cordycepin in the liver microsome while laying a methodological foundation for researching in-vivo and in-vitro metabolites of the cordycepin, and accordingly has a great significance.
Owner:LIAONING UNIVERSITY
Nitrogen-containing fused heterocyclic compound, as well as preparation method, intermediate, composition and application thereof
ActiveUS20190010153A1High selectivityStrong inhibitory activitySilicon organic compoundsGroup 5/15 element organic compoundsMetaboliteEnantiomer
The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
Owner:SHANGAI PHARMA GRP CO LTD
A method for liver microsomes to metabolize chlorinated paraffin in vitro
ActiveCN113533556BImprove metabolic clearanceFacilitate understanding of metabolic clearance rulesComponent separationMetabolic clearance rateOrganosolv
Owner:广东省农业科学院农业质量标准与监测技术研究所
Method for detecting metabolic performance of new chemical entity in different species of liver microsomes
ActiveCN112782336AImprove reliabilitySimple reaction conditionsComponent separationChemical methods analysisBiotechnologyNew medications
The invention discloses a method for detecting the metabolic performance of a new chemical entity in different species of liver microsomes, which comprises the following steps: in a reaction system containing a buffer solution, liver microsomes, a substrate, MgCl2 and NADPH, screening out an optimal reaction condition by taking the metabolic rate of the substrate as a reference to obtain a human liver microsome incubation system. According to the establishment method of the human liver microsome incubation system, rat, mouse, dog and monkey liver microsome incubation systems are sequentially established. The method comprises the following steps: performing in-vitro metabolism test on a new chemical entity in incubation systems of different species of liver microsomes, performing positive group reaction by using a substrate, and setting a negative group without adding NADPH and a blank group without adding liver microsomes; and identifying a metabolism result after testing. According to the method for detecting the metabolic performance of the new chemical entity in different species of liver microsomes, false positive and false negative results can be avoided, the reliability of an identification result is improved, and a reliable basis is provided for promoting research and development of new drugs.
Owner:安领生物医药(苏州)有限公司
Method for in-vitro metabolism of chlorinated paraffin by liver microsome
ActiveCN113533556AImprove metabolic clearanceFacilitate understanding of metabolic clearance rulesComponent separationMetabolic clearance rateOrganic solvent
The invention discloses a method for in-vitro metabolism of chlorinated paraffin by liver microsomes, which comprises the following steps: (1) dissolving chlorinated paraffin in an organic solvent to obtain a chlorinated paraffin solution, adding serum into the chlorinated paraffin solution, and standing for balancing to obtain a substrate system; (2) sequentially adding a potassium phosphate buffer solution, liver microsome and an NADPH enzyme regeneration system into the substrate system, uniformly shaking to obtain a final reaction system, and then putting the final reaction system into a water bath at 37 DEG C for oscillating reaction; and (3) adding an ice-colded organic solvent into the reaction system in the step (2) to terminate the reaction, then centrifuging the solution, taking a supernatant liquid, and measuring the content of chlorinated paraffin. The serum is adopted as a carrier of the chlorinated paraffin, and reaction of the chlorinated paraffin and the liver microsome is promoted, so that the metabolic clearance rate of the chlorinated paraffin is remarkably increased, and the measurement of the metabolic clearance rate of the liver microsome for in-vitro metabolism of the chlorinated paraffin is realized.
Owner:广东省农业科学院农业质量标准与监测技术研究所
2,4-Bis (trifluoroethoxy)pyridine compound and drug containing the compound
InactiveUS20050020606A1Good metabolic stabilityPromote oral absorptionOrganic active ingredientsOrganic chemistryOral medicationHydrogen atom
The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1): (wherein X1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and to a drug containing the compound or the salt as an active ingredient. The compound has metabolic resistance in human liver microsome, good absorbability upon oral administration, and excellent ACAT inhibitory activity.
Owner:KOWA CO LTD
LC-MC method used for determining NNK metabolites in liver microsomes
ActiveCN102445510BFast analysisGood choiceComponent separationMaterial analysis by electric/magnetic meansNitrosoNNK Metabolite
Owner:ZHENGZHOU TOBACCO RES INST OF CNTC
Nitrogen-containing fused heterocyclic compound, and preparation method, intermediate, composition and application thereof
ActiveCN108264512AStrong inhibitory activitySignificant inhibition of proliferationOrganic active ingredientsGroup 3/13 element organic compoundsCyclin-dependent kinase activityNitrogen
The invention discloses a nitrogen-containing fused heterocyclic compound, and a preparation method, an intermediate, a composition and an application thereof. The compound has a high inhibitory activity against different subtypes of CDK at the molecular level, has a good inhibitory activity against breast cancer cells at the cellular level, has a significant proliferation inhibition effect on tumor cells associated with the cyclin-dependent kinase activity at the animal level, and has the advantages of good stability of liver microsomes in humans and mice, no significant inhibition effect onmetabolic enzymes, good absorption properties in rats and mice, high bioavailability, and good drug-forming property.
Owner:SHANGAI PHARMA GRP CO LTD
UPLC/MS/MS detection method of 1-hydroxymidazolam concentration in liver microsome
InactiveCN105136962AImprove stabilityShorter Chromatography TimeComponent separationSpectrometerStandard curve
The invention discloses a UPLC / MS / MS detection method of the 1-hydroxymidazolam concentration in a liver microsome. The UPLC / MS / MS detection method comprises the following steps that 1, a liver microsome incubation system is established, serial concentrations of 1-hydroxymidazolam comparison products are added to prepare a standard curve sample; 2, the standard curve sample is injected into a UPLC / MS / MS liquid chromatograph / mass spectrometer for detection, and a standard 1-hydroxymidazolam curve is obtained according to the detection result; 3, a sample to be detected is prepared by adopting the same method as the step 1 and is injected into the UPLC / MS / MS liquid chromatograph / mass spectrometer, detection is performed under the same conditions as the step 2, and the 1-hydroxymidazolam concentration in the sample to be detected is obtained according to the standard curve. The UPLC / MS / MS detection method is short in analysis time, high in sensitivity and small in sample size, meets the methodological validation requirement, is suitable for determination of the 1-hydroxymidazolam concentration in the liver microsome incubation sample and has wide application prospect.
Owner:成都华西海圻医药科技有限公司
Microsomal bioreactor for synthesis of drug metabolites
InactiveUS20180044657A1Improve stabilityOxidoreductasesEnzyme production/based bioreactorsMetaboliteNiacinamide
Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.
Owner:BOARD OF REGENTS FOR OKLAHOMA STATE UNIVERSITY
Human liver microsome and cell co-culture system and construction method and application thereof
PendingCN113621557ASuppresses sources of bacterial contaminationDoes not affect growthArtificial cell constructsRespiratory/lung cellsBiotechnologyMicrobiology
The invention relates to a human liver microsome and cell co-culture system and a construction method and application thereof. Sterility of a human liver source is very difficult to ensure, and when human-derived liver microsome is prepared, the sterile liver microsome is hardly obtained. In order to carry out in-vitro metabolism test research on human-derived liver microsome and cell co-culture, the invention provides a co-culture method capable of enabling the germy human liver microsome to be in direct contact with sterile cells, and successfully constructs the human liver microsome and cell co-culture system. Tests prove that the construction method disclosed by the invention can ensure that pollution sources in the human liver microsome cannot influence the sterile environment of the cells, and the sterile state of normal growth of the cells is maintained. Moreover, the method is suitable for in-vitro metabolism research of allogenic substances (such as nicotine and smoke), and lays a foundation for in-vitro metabolism research of the combined action of the human-derived liver microsome and the cells.
Owner:ZHENGZHOU TOBACCO RES INST OF CNTC
Cocktail method for detecting activities of UGT (uridine diphosphoglucuronyl transferase) enzymes in liver microsome
The invention discloses a cocktail method for detecting activities of five UGT enzymes. The method comprises the following steps: selecting substrates with high specificity to the five UGT enzymes, setting a proper concentration, performing substrate interaction survey, mixing and incubating substrates of enzymes UGT1A1 / Ugt1a1 and UGT1A6 / Ugt1a6 with small interactions, mixing and incubating substrates of UGT1A3 / Ugt1a3, UGT1A9 / Ugt1a9 and UGT2B7 / AZTG, and finally measuring the activities of the UGT enzymes. The cocktail method for detecting the activities of the five UGT enzymes disclosed by the invention can be used for detecting the activities of UGT enzymes in rat and human liver microsome, has the advantages of high efficiency, rapidness and comprehensiveness and can be used for rapidly evaluating the influences of compounds on the activities of UGT enzymes.
Owner:EAST CHINA NORMAL UNIV
Novel application of qi-tonifying and heart-rate-restoring preparation for injection
The invention provides novel application of a qi-tonifying and heart-rate-restoring preparation for injection and especially to application of the qi-tonifying and heart-rate-restoring preparation for injection in preparing medicines exerting induction action on the activity of the liver microsomes, CYP1A2 and CYP3A4.
Owner:TIANJIN TASLY ZHIJIAO PHARMA
Deuterated 1, 4-benzodiazepine-2, 5-diketone compound and application thereof
PendingCN114507190APromote degradationSlow growth rateOrganic active ingredientsIsotope introduction to organic compoundsBenzodiazepineDiketone
The invention discloses a deuterated 1, 4-benzodiazepine-2, 5-diketone compound and an application of the deuterated 1, 4-benzodiazepine-2, 5-diketone compound. The invention provides a compound shown as a formula I or pharmaceutically acceptable salt thereof. The 1, 4-benzodiazepine-2, 5-diketone active compound keeps the activity of inhibiting tumor cells and tumor stem cells, the degradation effect of in-vitro human liver microsome on the compound is prolonged, the half-life period is obviously prolonged, and a safer and more reliable candidate is provided for developing novel anti-tumor drugs.
Owner:NINGBO COMBIREG PHARMA TECH CO LTD
Heterocyclic compound and application thereof
ActiveCN113880843AStrong inhibitory activityGood metabolic stabilityOrganic active ingredientsNervous disorderMetabolic stabilityPharmaceutical medicine
The invention discloses a heterocyclic compound and application thereof. The invention specifically discloses a heterocyclic compound as shown in a formula I, and a tautomer or pharmaceutically acceptable salt thereof. The compound has better inhibitory activity on TRPC5, has better metabolic stability in liver microsome, and has better clinical pharmacokinetic properties.
Owner:WUHAN LL SCI & TECH DEV
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