RIPK1-IN-11,2173557-02-1

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RIPK1-IN-11

CAS No. : 2173557-02-1

MCE 国际站：RIPK1-IN-11

产品活性：RIPK1-IN-11是一种口服有效的RIPK1抑制剂 (K_d=9.2 nM; IC₅₀=67 nM)，可抑制人和小鼠细胞坏死。具有抗炎活性。

研究领域：Apoptosis

作用靶点：RIP kinase

In Vitro: RIPK1-IN-11 (compound 70) (24 hours; for 1h prior to the treatment of TNFα) efficiently blocks necroptosis induced by TNFα in both human and mouse cells (EC₅₀=17-30 nM).
Pharmacokinetic profiles of compound 70 in male SD rats

	IV (2 mg/kg)	PO (10 mg/kg)
Tmax (h)		1.2
Cmax (ng/mL)	1330	1241
AUC0-24 (ng/mL∗h)	1208	3827
t1/2 (ng/mL)	1.0	1.7
CL (mL/min/kg)	33
Vd, ss (L/kg)	2.4
F (%)		63%

In Vivo: RIPK1-IN-11 (3 mg/kg; i.p. for 30 min, followed by injection with TNFα) blocks hypothermia and death in mice in the TNFα-induced SIRS model.
RIPK1-IN-11 (5 mg/kg, 25 mg/kg; p.o.; 7 days; C57BL/6 mouse) exhibits no obvious toxicity in mice.

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