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JNJ-42041935
缺氧诱导因子(HIF)脯氨酰羟化酶(PHD)抑制剂

JNJ-42041935

产品编号:C4752
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Sample solution is provided at 25 µL, 10mM.

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批次:

化学结构

JNJ-42041935

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化学性质

CAS号 1193383-09-3 SDF Download SDF
别名 HIF-PHD Inhibitor II
化学名 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-1H-pyrazole-4-carboxylic acid
SMILES ClC1=CC2=C(NC(N3C=C(C(O)=O)C=N3)=N2)C=C1OC(F)(F)F
分子式 C12H6ClF3N4O3 分子量 346.7
溶解度 ≤10mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide 储存条件 Store at -20°C
物理性状 A crystalline solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

产品描述

pKI: 7.3-7.9

JNJ-42041935 is a Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor.

The hypoxia-inducible factor prolyl hydroxylase enzymes have been considered as novel targets for the treatment of ulcerative colitis, anemia, ischemic and metabolic disease inter alia. In addition, hypoxia-inducible factor prolyl hydroxylase enzymes act as central gatekeepers of posttranscriptional and transcriptional adaptation to hypoxia, oxidative stress, as well as excitotoxicity.

In vitro: In a previou study, the pharmacology of JNJ-42041935 was investigated in both enzyme and cellular and was compared with other compounds described in the literature as PHD inhibitors. Results showed that JNJ-42041935 was a selective, potent, 2-oxoglutarate competitive and reversible inhibitor of PHD enzymes [1].

In vivo: In animal study, JNJ-42041935 was used to compare the effect of selective inhibition of PHD to intermittent, high doses (50 μg/kg i.p.) of an exogenous erythropoietin receptor agonist in an inflammation-induced anemia model in rats. Results showed that daily JNJ-42041935 treatment at 100 μmol/kg for 14 days was effective in reversing inflammation-induced anemia, while erythropoietin had no effect [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Barrett, T. D.,Palomino, H.L.,Brondstetter, T.I., et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Molecular Pharmacology 79(6), 910-920 (2011).