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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-JNJ-42041935
JNJ-42041935

Chemical Structure : JNJ-42041935

CAS No.: 1193383-09-3

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JNJ-42041935 (JNJ42041935)

货号: PC-43241Not For Human Use, Lab Use Only.

JNJ-42041935 is a potent, selective, 2-OG-competitive, reversible inhibitor of HIF-PHD with pKi of 7.91, 7.29 and 7.65 for PHD1, PHD2 and PHD3, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-42041935 is a potent, selective, 2-OG-competitive, reversible inhibitor of HIF-PHD with pKi of 7.91, 7.29 and 7.65 for PHD1, PHD2 and PHD3, respectively.
JNJ-42041935 shows highly selectivity for PHD relative to FIH (pIC50=4.0).
JNJ-42041935 is approximately equipotent in the HIF-1α accumulation and erythropoietin secretion assays in Hep3B cells as DMOG and 3,4-EDHB.
JNJ-42041935 reverses inflammation-induced anemia at dose of 100 μmol/kg, whereas erythropoietin has no effect.

物理化学性质&存储条件

分子量 346.6493
分子式 C12H6ClF3N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 36 mg/mL
Chemical Name/SMILES

1H-Pyrazole-4-carboxylic acid, 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-

参考文献

1. Barrett TD, et al. Mol Pharmacol. 2011 Jun;79(6):910-20.

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