79 results about "Bifunctional chelator" patented technology

The invention relates to an RGD polypeptide radiopharmaceutical and a preparation method thereof. The RGD polypeptide radiopharmaceutical includes an RGD polypeptide and a radionuclide<99m>Tc, wherein, the RGD polypeptide radiopharmaceutical is an RGD cyclopeptide dimmer, that is, E(L-cRGDxK)2 which is synthesized by dimerizing two RGD polypeptide monomers connected with coupling agent L. The radionuclide<99m>Tc serves to mark the RGD cyclopeptide dimmer through a bifunctional chelating agent HYNIC. A pharmacokinetics modified molecule PKM is further connected between the RGD cyclopeptide dimmer and the bifunctional chelating agent. The RGD polypeptide radiopharmaceutical is <99m>Tc-HYNIC-PKM-E(L-cRGDxK)2. The RGD polypeptide radiopharmaceutical is colorless and transparent liquid injection. The RGD polypeptide radiopharmaceutical provided by the invention has the advantages of further reinforcing the binding affinity and the ingestion of drugs by tumor, and achieving better diagnosis effect.

The invention relates to a radionuclide-marked RGD polypeptide medicine and a preparation method thereof. The medicine comprises RGD polypeptide, a bifunctional Chelator and radioactive Nuclide, wherein the RGD polypeptide is RGD cyclic peptide dimer, namely E(L-c(RGDxK))2, which is synthesized by connecting a connecting agent L and an RGD polypeptide monomer and dimerizing two RGD polypeptide monomers connected with the connecting agent L; the radioactive Nuclide marks the RGD cyclic peptide dimer through the bifunctional Chelator; and a pharmacokinetic modified molecule PKM is also connected between the RGD cyclic peptide dimer and the bifunctional Chelator. The radionuclide-marked RGD polypeptide medicine is Nuclide-Chelator-PKM-E(L-c(RGDxK))2, and is a colorless and transparent liquid injection solution. The radionuclide-marked RGD polypeptide medicine is used for diagnosing and treating integrin alpha v beta 3 positive tumor.

The invention provides a rapid detection method for mercury in a liquid biological sample based on magnetic separation and quantum dots (QDs) marking. The method comprises the steps: (1) preparing mercury-resistant monoclonal antibodies; (2) coupling the mercury-resistant monoclonal antibodies with magnetic nanobeads through covalent bonds to prepare mercury-resistant immunomagnetic nanobeadd; and (3) adding a difunctional chelating agent, bovine serum albumin (BSA) and triethylamine (TEA) into the liquid biological sample to incubate, then, adding the mercury-resistant immunomagnetic nanobeads to sufficiently mix, next, carrying out magnetic separation, and adding biotinylated BSA antibodies and streptavidinylated QDs into a sediment, and carrying out fluorescence detection by using a fluorescence microplate, wherein the sediment is obtained through magnetic separation. The invention also provides a rapid detection kit for mercury in a liquid biological sample.

The invention relates to an NGR (asparagine-glycine-arginine) polypeptide radiopharmaceutical as well as a preparation method and application thereof. The currently reported radionuclide-labeled NGR-containing sequence has a higher liver uptake rate. The NGR polypeptide radiopharmaceutical is formed with the preparation method comprising the steps as follows: monomers and dimmers of an NGR cyclopeptide are connected with a chelating agent NOTA to form a coordination compound, and the coordination compound finally forms the radiopharmaceutical through chelation of the NOTA (disodium edta) and radionuclides; the targeting action of the NGR polypeptide enables the radiopharmaceutical to be concentrated to a tumor part, and the nuclear medicine positron emission computerized tomography technology is utilized to image the CD13 positive tumor, so as to achieve the purpose of specific diagnosis. According to the invention, since the NOTA is used as a bifunctional chelator to be chelated with the radionuclides, and the p-SCN-Bn is used as a coupling agent to enable the NGR to be directly connected to a carbon skeleton of the NOTA, the situation that the coordination of the carboxyl oxygen atoms and the radionuclides is influenced by connection of the coupling agent and the NOTA carboxyl is avoided; seen from the metabolism in vivo, the radiopharmaceutical can be quickly metabolized through the kidney after being injected into the body, and the liver uptake rate is lower.

The present invention relates to a method for preparing a bifunctional chelator for lanthanide. The method comprises the steps of providing a starting material which has an amino and carboxyl group; protecting the amino with an amino protecting group and the carboxyl with a carboxyl protecting group to produce a protected compound; reacting the protected compound with cyclen to generate a monoalkylated cyclen; reacting the monoalkylated cyclone with an activated compound to generated tetra-alkylated cyclone; removing the amino protecting group with a first protecting group removal reagent; and removing the carboxyl protecting groups with a second protecting group removal reagent to yield a bifunctional chelator having three more carboxyl groups and one or more amino groups.

A compound fur radio metal complexation includes a chelator and one or more biological targeting vectors TV conjugated to said chelator, wherein the chelator has structure (A) or (B)or (C).based on 1,4-diazepine with groups R1, R2, R3, R4, X1, X2, X3. The compound is particularly suited for complexation of radio-isotopic metals, such as 66Ga(III), 67Ga(III) and 68Ga(III).

A method for reducing odor is provided. In one embodiment, the method comprises forming a coordination complex between particles having a positive zeta potential and a transition metal. The method further comprises contacting the coordination complex with an odorous compound, the transition metal providing one or more active sites for capturing the odorous compound. For example, in one embodiment, the particles are formed from alumina-coated silica. In addition, the coordination complex may be formed using a bifunctional chelating agent.

A bifunctional chelating agent of the formula (I):wherein the variables R1, R1′, Q1, Q2 and M are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a stable or radioactive metal; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate.

The invention discloses a Dar2 polypeptide radioactive drug and a preparation method thereof. The drug comprises a Dar polypeptide dimer and a radioactive nuclide, wherein the radioactive nuclide canmark the Dar polypeptide dimer through a bifunctional chelating agent; the Dar polypeptide dimer is a polypeptide dimer which is synthesized through the steps of enabling GGG to be connected with twoDar polypeptide monomers and performing dimerization on the two Dar polypeptide monomers connected to the GGG; and each Dar polypeptide monomer is D type amino acid linear heptatomic polypeptide, andthe sequence is anedywr. According to the drug disclosed by the invention, the radioactive nuclide is marked on Dar polypeptide dimer molecules through the bifunctional chelating agent, the in vivo marked drug is concentrated to tumor positions through the targeting effects of Dar polypeptide, and through a single-photon emission computed tomography (SPECT) technique or a positron emission computed tomography (PET) technique of nuclear medicine, tomography diagnosis is performed on integrin alpha 6 positive tumor.

Chelants and macrocyclic metal complexes thereof, methods of preparing the chelants and macrocyclic metal complexes, and radiopharmaceutical compositions comprising the macrocyclic metal complexes are disclosed. Methods of using the macrocyclic metal complexes as radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious diseases and cancer are also disclosed. Chelants as bifunctional chelators (BFCs) for the radiolabeling of target-specific biomolecules, such as proteins, peptides, peptidomimetics, non-peptide receptor ligands, enzyme inhibitors, and enzyme substrates are disclosed. Methods of using macrocyclic metal complexes containing the chelant-biomolecule conjugates as target-specific diagnostic radiopharmaceuticals that selectively localize at sites of disease and allow an image to be obtained of the loci using gamma scintigraphy are disclosed. Methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders, such as thromboembolic disease or atherosclerosis, infectious disease and cancer are further disclosed.

The invention discloses a method for preparing heavy metal holoantigen with high coupling rate and high activity. The method is implemented by improving the synthetic sequence of the heavy metal holoantigen and comprises the following steps of: reacting superfluous heavy metal ion with bifunctional chelator completely, regulating the pH value by using a NaOH solution; performing centrifugal precipitation; removing the superfluous heavy metal ion to obtain a metal ion and chelator compound, so that the metal ion and chelator compound cannot be well reacted with a biomacromolecule; coupling the metal ion and chelator compound with carrier protein, so that the activity of protein in the prepared holoantigen is guaranteed; and thus obtaining the holoantigen with high coupling rate and high activity. Immune tests in mice prove that the prepared holoantigen has high immunogenicity and is simple and practicable, and the preparation method has high repeatability.

The invention relates to an arginyl-glycyl-aspartic acid (RGD) polypeptide radioactive medicine and preparation method thereof for intergrin alpha-v-beta3 receptor positive tumor diagnosis. The medicine is a galactosed RGD cyclic dimer in structure, and the medicine is subjected to a radionuclide 99mTc labeling through a bifunctional chelator hydrazino nicotinamide (HYNIC). The medicine is characterized in that two galactoses are used as a joining chain of the RGD, the uptaking of the medicine in non-target organs of intestinal canal, lungs and the like is reduced, and thereby the image quality of tumor imaging is improved. The radioactive medicine is 99mTc-Galacto-RGD2 and is a colorless transparent liquid injection.

The invention provides a synthesis method for preparing a heavy metal lead artificial antigen based on a novel difunctional chelating agent DOTA (2-S-(4-amino-benzene)-1,4,7,10-tetraazacyclononane-1,4,7,10-tetraacetic acid). According to the preparation method, DOTA is taken as the chelating agent, a lead ion chelating agent compound is coupled with BSA (bovine serum albumin) as carrier protein orKHL (human serum albumin), and the artificial antigen is prepared. According to the method, the step of sodium borohydride reduction is added on the original traditional basis, so that the coupling efficiency is improved. The invention further provides an application of DOTA to preparation of the heavy metal lead artificial antigen.

The invention provides a TSH (thyroid stimulating hormone) quantitative detection kit based on time-resolved fluoroimmunoassay, applicable to clinical screening of neonatal hypothyroidism. The preparation method of the kit is characterized by comprising the following steps of: 1, separating an antibody conjugate (Eu-Anti-TSH) from free rare earth ions (Eu<3+>) by using a specific chromatograph column; (2) using a bifunctional chelator (DTTA) for marking, wherein one end of the bifunctional chelator is chelated with rare earth ions (Eu) and the other end of the bifunctional chelator is connected with -NH2 of protein; adding beta-NTA to reinforcing liquid and regulating the concentration so that the fluorescence intensity of a finally obtained reagent is improved; and (4) adding a substitute Proclin300 for sodium azide to an analysis buffer system. Based on the characteristics of the steps in the preparation method, the TSH quantitative detection kit based on time-resolved fluoroimmunoassay can be produced and other in vitro diagnosis detection reagents can be developed.

The present invention relates to a method for preparing a bifunctional chelator for lanthanide. The method comprises the steps of providing a starting material which has an amino and carboxyl group; protecting the amino with an amino protecting group and the carboxyl with a carboxyl protecting group to produce a protected compound; reacting the protected compound with cyclen to generate a monoalkylated cyclen; reacting the monoalkylated cyclone with an activated compound to generated tetra-alkylated cyclone; removing the amino protecting group with a first protecting group removal reagent; and removing the carboxyl protecting groups with a second protecting group removal reagent to yield a bifunctional chelator having three more carboxyl groups and one or more amino groups.