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CAS No.: 1558021-37-6

TP0463518 Catalog No. CSN24188

Synonyms: TP0463518

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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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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^[2].
作用机制TP0463518 competitively inhibits PHD.^[2]
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.
参考文献

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.

[1] Kato S, Takayama N, et al. TP0463518, a novel inhibitor for hypoxia-inducible factor prolyl hydroxylases, increases erythropoietin in rodents and monkeys with a good pharmacokinetics-pharmacodynamics correlation. Eur J Pharmacol. 2018 Nov 5;838:138-144.
[2] Kato S, Takayama N, Takano H, Koretsune H, Koizumi C, Kunioka EI, Uchida S, Takahashi T, Yamamoto K. TP0463518, a novel inhibitor for hypoxia-inducible factor prolyl hydroxylases, increases erythropoietin in rodents and monkeys with a good pharmacokinetics-pharmacodynamics correlation. Eur J Pharmacol. 2018 Nov 5;838:138-144. doi: 10.1016/j.ejphar.2018.08.044. Epub 2018 Sep 1. PMID: 30179610.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3157 mL
- 11.5787 mL
- 23.1575 mL
- 5 mM
- 0.4631 mL
- 2.3157 mL
- 4.6315 mL
- 10 mM
- 0.2316 mL
- 1.1579 mL
- 2.3157 mL

技术信息

CAS号

1558021-37-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H18ClN3O6

运输

蓝冰

分子量

431.83

别名

TP0463518

溶解度

DMSO	420.0 mg/mL (972.6 mM)
Water	insoluble

动物实验配方

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