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HIF-PHD Inhibitor II, JNJ-42041935-Calbiochem

品牌
Sigma-Aldrich
货号
400093
规格纯度
The HIF-PHD Inhibitor II, JNJ-42041935 controls the biological activity of HIF-PHD. This small molecule/inhibitor is primarily used for Cell Structure applications.
参考价格
3736.22 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.
A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Lee, K., et al., 2013. Angew. Chem. Int. Ed.52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol.79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C12H6ClF3N4O3
分子量346.65
MDL编号MFCD28900740

产品性质

质量水平100
测定≥99% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 100 mg/mL
运输ambient
储存温度2-8℃
SMILES stringClC1=CC2=C(NC(N3C=C(C=N3)C(O)=O)=N2)C=C1OC(F)(F)F

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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