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

RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor ( K d =9.2 nM; IC 50 =67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC 50 =17-30 nM). Anti-inflammatory activity [1].

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 (EC 50 =17-30 nM) [1]. Pharmacokinetic profiles of compound 70 in male SD rats IV (2 mg/kg) PO (10 mg/kg) T max (h) 1.2 C max (ng/mL) 1330 1241 AUC 0-24 (ng/mL h) 1208 3827 t 1/2 (ng/mL) 1.0 1.7 CL (mL/min/kg) 33 Vd, ss (L/kg) 2.4 F (%) 63%

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 [1]. RIPK1-IN-11 (5 mg/kg, 25 mg/kg; p.o.; 7 days; C57BL/6 mouse) exhibits no obvious toxicity in mice [1]. Animal Model: C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome) [1] Dosage: 3 mg/kg Administration: i.p. for 30 min, followed by injection with TNFα (0.25 μg/g) Result: Significantly reduced TNFα-induced temperature loss and ameliorated lethal shock in mice.

2173557-02-1

C23H24N4O4S

452.53

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years