AbMole| JNJ-42041935(CAS号1193383-09-3;目录号M8963)

摘要:JNJ-42041935是一种高效的,竞争性的,选择性脯氨酰羟化酶PHD抑制剂,对于PHD1, PHD2 and PHD3的pKi值分别为7.91±0.04,7.29 ±0.05和7.65±0.09。

JNJ-42041935是一种高效的,竞争性的,选择性脯氨酰羟化酶PHD抑制剂,对于PHD1, PHD2 and PHD3的pKi值分别为7.91±0.04,7.29 ±0.05和7.65±0.09。

生物活性

JNJ-42041935是一种有效的,2-氧戊二酸竞争性,可逆性和选择性PHD酶抑制剂。JNJ-42041935是PHD2181-417最有效的抑制剂,其pIC50的值为7.0±0.03。JNJ-42041935(100 μmol/kg,每天一次,持续14天)能有效逆转炎症诱导的贫血。


实验参考

体外实验*

细胞系 Hep3B cells

方法 The potency of compounds for stabilization of intracellular HIF-1α and release of erythropoietin into the media was assessed in the human hepatoma cell line Hep3B. Cells were cultured in Dulbecco's modified Eagle's medium/high glucose (Invitrogen) supplemented with 10% fetal calf serum and 2 mM l-glutamine, 1% nonessential amino acids, 1 mM sodium pyruvate, 50 IU/ml penicillin, and 50 μg/ml streptomycin. A range of concentrations was incubated in 96-well plates with 30,000 cells/well for 24 h. Incubation media were collected, and cells were subsequently lysed for assessment of cellular HIF-1α content and erythropoietin concentration.

浓度 1 to 10 μM

处理时间 24 h

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*

动物模型 Balb/C mice

配制

剂量 30, 100, and 300 μmol/kg

给药处理 p.o.

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。


化学性质

分子量 346.65

CAS号 1193383-09-3

溶解性(25°C) DMSO ≥ 30 mg/mL

储存条件 粉末型式 -20°C 3年;4°C 2年

溶于溶剂 -80°C 6个月;-20°C 1个月

运输方式 冰袋运输,根据产品的不同,可能会有相应调整。


储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg

1 mM 2.8848 mL 14.4238 mL 28.8475 mL

5 mM 0.577 mL 2.8848 mL 5.7695 mL

10 mM 0.2885 mL 1.4424 mL 2.8848 mL


参考文献

[1] Corcoran A, et al. Hippocampus. A role for prolyl hydroxylase domain proteins in hippocampal synaptic plasticity.

[2] Barrett TD, et al. Mol Pharmacol. 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.

来源:AbMole

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