PHD-1-IN-1 是一种具有口服活性的，有效的缺氧诱导因子脯氨酰羟化酶结构域 1 (PHD-1) 抑制剂，IC50 为 0.034 μM。PHD-1-IN-1 与活性位 Fe2+ 具有独特的单齿结合相互作用，并诱导形成一个 “Arg367-out” 口袋。
货号:ajcx37900
CAS:2009343-14-8
分子式:C13H8N4
分子量：220.23
溶解度:DMSO : 195 mg/mL (885.44 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an "Arg367-out" pocket[1].

PHD-1-IN-1 (compound 17; 3 mg/kg of p.o. or 0.5 mg/kg of i.v.) has a Cmax of 0.8 μM, a AUC of 176 ng•h/mL, Kp,uu of 1.11 and B/P of 0.95[1].

[1]. Ahmed S, et al. 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction. J Med Chem. 2017 Jul 13;60(13):5663-5672.