PHD2-IN-1_product_DataBase

Bioactivity	PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research[1].
Invitro	PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 小时) 稳定 HIF-α 并增加促红细胞生成素 (EPO) 基因的表达。 RT-PCR[1] Cell Line:
In Vivo	PHD2-IN-1 (Compound 22) (10,20,50 mg/kg 口服，每日一次持续三天) 在 C57BL/6 小鼠中刺激红细胞生成并以剂量依赖性方式增加网织红细胞[1]。PHD2-IN-1 (50,100,200 mg/kg，腹腔注射, 每日一次持续三天) 对 ICR 小鼠无明显毒性反应[1]。PHD2-IN-1 (静脉注射1 mg/kg，口服10 mg/kg) 显示在大鼠中 T1/2 为 2.29 小时 (口服) 或 3.72 小时 (静脉注射)，在小鼠中 T1/2 为 1.17 小时 (口服) 或 0.33 小时 (静脉注射)。在大鼠和小鼠中的口服生物利用度 (F%) 分别为 33.9% 和 35.3%[1]。 Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice [1]Species
Name	PHD2-IN-1
CAS	2768219-28-7
Formula	C21H23ClN4O5
Molar Mass	446.88
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Wu Y, et.al. Preferred Conformation-Guided Discovery of Potent and Orally Active HIF Prolyl Hydroxylase 2 Inhibitors for the Treatment of Anemia. J Med Chem. 2023 Jul 13;66(13):8545-8563.

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