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编 号：F749624
分子式：C23H24N4O4S
分子量：452.53
分子式：C23H24N4O4S
分子量：452.53
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CAS No: 2173557-02-1
产品详情
生物活性：
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity.
体内研究：
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.Animal Model:C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome)
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.
体外研究：
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 ratsIV (2 mg/kg) PO (10 mg/kg)
Tmax (h)1.2
Cmax (ng/mL)13301241
AUC0-24 (ng/mL?h)12083827
t1/2 (ng/mL)1.01.7
CL (mL/min/kg)33
Vd, ss (L/kg)2.4
F (%)63%
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity.
体内研究：
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.Animal Model:C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome)
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.
体外研究：
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 ratsIV (2 mg/kg) PO (10 mg/kg)
Tmax (h)1.2
Cmax (ng/mL)13301241
AUC0-24 (ng/mL?h)12083827
t1/2 (ng/mL)1.01.7
CL (mL/min/kg)33
Vd, ss (L/kg)2.4
F (%)63%
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