CAS:1558021-37-6TP0463518

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TP0463518 is a potent HIF-PHD inhibitor with Ki value of 5.3 nM for PHD2, and also inhibited human PHD1/3 with IC50 values of 18 and 63 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1558021-37-6

储存条件

分子式

C20H18ClN3O6

运输

蓝冰

分子量

431.83

别名

溶解度

DMSO	420.0 mg/mL (972.6 mM)
Water	insoluble

动物实验配方

生物活性

描述TP0463518 is a novel PHD inhibitor with IC50 values of 18/5.3/63nM for PHD1/2/3. It increased erythropoietin in rodents and monkeys with a good pharmacokinetics-pharmacodynamics correlation. In normal mice and rats, TP0463518 significantly increased the serum EPO levels at doses of 5 and 20 mg/kg, respectively. In normal mice and rats, TP0463518 significantly increased the serum EPO levels at doses of 5 and 20 mg/kg, respectively. It also increased the serum EPO level in 5/6 nephrectomized chronic kidney disease model rats at a dose of 10 mg/kg.
作用机制TP0463518 competitively inhibits PHD.^[1]
动物研究
剂量
Mice: 5 mg/kg - 40 mg/kg^[1] (p.o.) Rat: 1.25 mg/kg - 160 mg/kg^[1] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 5 mg/kg - 40 mg/kg^[1] (p.o.) Rat: 1.25 mg/kg - 160 mg/kg^[1] (p.o.)
给药途径	p.o.