Enarodustat hydrochloride_product_DataBase

Bioactivity	Enarodustat hydrochloride is a potent and orally active HIF/HIF Prolyl-Hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat hydrochloride has the potential for renal anemia treatment.
Target	pKi : 8.2 (5-HT2A receptor), 8.0 (D4 receptor), 6.7 (D2 receptor), 7.2 (α1 receptor), 6.9 (5-HT2C receptor), 5.7 (H1 receptor)
Invitro	Enarodustat hydrochloride (JTZ-951) 是一种有效的、具有口服活性的低氧诱导因子脯氨酰羟化酶抑制剂，EC50 为 0.22 μM。Enarodustat hydrochloride 既不显示 CYP（IC50 > 100 μM；CYP3A4/5、CYP2C9、CYP2D6、CYP1A2、CYP2A6、CYP2C19、CYP2C8、CYP2B6）也不显示 hERG（IC50 > 100 μM) 抑制[1]。
In Vivo	Enarodustat hydrochloride（1 和 3 mg/kg，口服）在大鼠中以剂量依赖的方式增加血红蛋白水平，每天口服给药[1]。
Name	Enarodustat hydrochloride
CAS	1262131-60-1
Formula	C17H17ClN4O4
Molar Mass	376.79
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]. Ogoshi Y, et al. Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325.

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