PHD2-IN-1,2768219-28-7

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PHD2-IN-1

CAS No. : 2768219-28-7

MCE 国际站：PHD2-IN-1

产品活性：PHD2-IN-1 是一种强效的、具有口服活性的 HIF-脯氨酰羟化酶2 (PHD2) 抑制剂，IC₅₀ 为 22.53 nM，可用于贫血病研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：HIF/HIF Prolyl-Hydroxylase

In Vitro: PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 hours) stabilizes HIF-α and increases the expression of the erythropoietin (EPO) gene.

In Vivo: PHD2-IN-1 (Compound 22) (10,20,50 mg/kg, p.o., once daily for three days) stimulates erythropoiesis and increase reticulocytes in a dose-dependent manner in C57BL/6 mice.
PHD2-IN-1 (50,100,200 mg/kg for i.p., once daily for 14 days) has no significant toxic reactions in ICR mice.
PHD2-IN-1 (1 mg/kg for i.p., 10 mg/kg for p.o.) shows T_1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice.
Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice

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Species	Route	Dose (mg/kg)	Tmax (h)	Cmax (ng/mL)	AUC0-t (h•ng/mL)	AUC0-Ꝏ (h•ng/mL)	T1/2 (h)	CL (mL•min-1/kg-1)	VZ (mL/kg)	MRT0-Ꝏ (h)	F (%)
rat	p.o.	10	0.08	26140	7118	7135	2.29	1417	4629	0.56	33.9
rat	i.v.	1	/	/	2069	2106	3.72	483	2644	1.54	/
mice	p.o.	10	0.5	3036	4475	4489	1.17	2246	4532	1.67	35.3
mice	i.v.	1	/	/	1384	1387	0.33	721	345	0.53	/