A kind of 1,2,3-propanetriacid-coupled epo peptidomimetic derivative and its preparation method and application
A technology of glyceric acid coupling and peptide derivatives, applied in 1, can solve the problems of low EC50 and limitations, and achieve the effect of prolonging half-life
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Embodiment 1
[0045] Example 1 Synthesis of Dimers of Erythropoietin Peptidomimetic Derivatives
[0046] The erythropoietin peptidomimetic of the present invention is a polypeptide, which can be prepared by using the Fmoc solid-phase polypeptide synthesis method, and the CS 336X instrument produced by CSBio Company to synthesize the polypeptide of the present invention. The method of synthesis was carried out according to the manufacturer's instruction manual. The Fmoc solid-phase polypeptide synthesis method described herein refers to a synthetic method in which a polymer resin is used as a solid-phase reaction matrix to sequentially condense amino-terminal Fmoc-protected amino acids in the presence of a coupling reagent to synthesize a polypeptide. x 3 The carboxyl group is attached to the polymer resin, X 3 The amino group is condensed with the 2-position carboxyl group of 1,2,3-propanetriacic acid, and the 1- and 3-position carboxyl groups are respectively condensed with the side cha...
Embodiment 2
[0047] Example 2 Effects of dimers of erythropoietin peptidomimetic derivatives on mice
[0048] Using mice to evaluate and compare the effects of 1, 2, 3-propanetrilic acid-coupled erythropoietin peptidomimetic dimers and erythropoietin protein on mouse erythropoiesis.
[0049] Among them, EPO drugs were purchased from Shenyang Sansheng Pharmaceutical Co., Ltd.;
[0050] Kunming mice, purchased from Shanghai Experimental Animal Center of Chinese Academy of Sciences, weighing 25-30 g, are all female mice. The number of animals in each group in the experiment: 10, divided into 4 groups.
[0051] Among them, the mice in group 1 were injected with erythropoietin peptidomimetic derivative dimer coupled with 1, 2, 3 glyceric acid at a dose of 4.5 mg / kg, and the mice in group 1 were injected with erythropoietin protein at a dose of 4.5 mg / kg. 4.5mg / kg, the mice in group 1 were blank control, injected with PBS buffer solution for seven consecutive days, then sacrificed the mice, t...
Embodiment 3
[0055] Example 3: Effects of dimers of erythropoietin peptidomimetic derivatives on rhesus monkeys
[0056] The EPO drug used in the present invention was purchased from Shenyang Sansheng Pharmaceutical Co., Ltd.
[0057] Rhesus monkeys were used to evaluate the effect of dimers of erythropoietin peptidomimetic derivatives on erythropoiesis. Rhesus monkeys, weighing 5.5-8.5 kg, male or female, were purchased from Hainan Experimental Animal Center. The macaques were divided into two groups according to the basic hemoglobin, with three monkeys in each group. One group uses the dimer of the peptidomimetic derivatives of the present invention, intravenous injection once a week, 4.5 mg / kg each time; the other group uses EPO as the positive control group, three times / week, 1.5 mg / kg each time, continuously The drug was given for five weeks, and hematological indicators were measured once a week.
[0058] It was found that a single intravenous injection of the peptidomimetic deri...
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