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编 号：F755720
分子式：C28H28N6O2
分子量：480.56
分子式：C28H28N6O2
分子量：480.56
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CAS No: 2763831-53-2
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生物活性：
RI-962 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor. RI-962 inhibits RIPK1 with an IC50 value of 35.0?nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases.
体内研究：
RI-962 (i.p.; 40?mg/kg; once a day for 10 day) ameliorates TNFα-induced SIRS and reduces inflammation in acute DSS-induced colitis.Pharmacokinetic Parameters of RI-962 in rats (i.v., i.p., p.o.; 5, 20?mg/kg) .RI-962 i.v. p.o. i.p.
Dose (mg/kg)52020
T1/2 (h)2.1?±?0.21.3?±?0.28.5?±?1.6
Tmax (h)0.1?±?0.00.8?±?1.00.5?±?0.0
Cmax (ng/mL)12170.4?±?1198.5674.2?±?424.73603.3?±?693.3
AUC0–t(ng*h/mL)4526.1?±?546.01594.9?±?891.86459.7?±?1131.6
AUC0–∞ (ng*h/mL)4538.1?±?546.31604.5?±?896.16609.3?±?1121.4
Vss (L/kg)0.4?±?0.1--
MRT0–∞ (h)0.4?±?0.01.8?±?0.22.8?±?0.1
CL (mL/min/kg)18.5?±?2.1--
F (%)-8.8?±?5.035.7?±?6.3Animal Model:C57BL/6 female mice
Dosage:40?mg/kg
Administration:Intraperitoneal for 15?min; once a day for 10 day
Result:Ameliorated TNFα-induced SIRS by inhibiting RIPK1 activity.Suppressed the RIPK1 signaling in the mouse model of DSS-induced colitis.
Animal Model:Sprague-Dawley (SD) rats
Dosage:5, 20?mg/kg
Administration:intravenous (i.v.) (5?mg/kg), intraperitoneal (i.p.) (20?mg/kg) and oral (p.o.) (20?mg/kg)
Result:Had good metabolic stability in rats.
体外研究：
RI-962 has potent inhibitory activity for RIPK1 with an IC50 value of 35.0?nM.RI-962 has protective effect for necroptotic death with EC50 values of 10.0 nM, 4.2 nM, 11.4 nM, and 17.8?nM for HT29, L929, J774A.1, and U937 cells, respectively.RI-962 (0-100 μM; 24 h) protectes cells from TSZ-induced necroptosis by inhibiting the kinase activity of RIPK1.
RI-962 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor. RI-962 inhibits RIPK1 with an IC50 value of 35.0?nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases.
体内研究：
RI-962 (i.p.; 40?mg/kg; once a day for 10 day) ameliorates TNFα-induced SIRS and reduces inflammation in acute DSS-induced colitis.Pharmacokinetic Parameters of RI-962 in rats (i.v., i.p., p.o.; 5, 20?mg/kg) .RI-962 i.v. p.o. i.p.
Dose (mg/kg)52020
T1/2 (h)2.1?±?0.21.3?±?0.28.5?±?1.6
Tmax (h)0.1?±?0.00.8?±?1.00.5?±?0.0
Cmax (ng/mL)12170.4?±?1198.5674.2?±?424.73603.3?±?693.3
AUC0–t(ng*h/mL)4526.1?±?546.01594.9?±?891.86459.7?±?1131.6
AUC0–∞ (ng*h/mL)4538.1?±?546.31604.5?±?896.16609.3?±?1121.4
Vss (L/kg)0.4?±?0.1--
MRT0–∞ (h)0.4?±?0.01.8?±?0.22.8?±?0.1
CL (mL/min/kg)18.5?±?2.1--
F (%)-8.8?±?5.035.7?±?6.3Animal Model:C57BL/6 female mice
Dosage:40?mg/kg
Administration:Intraperitoneal for 15?min; once a day for 10 day
Result:Ameliorated TNFα-induced SIRS by inhibiting RIPK1 activity.Suppressed the RIPK1 signaling in the mouse model of DSS-induced colitis.
Animal Model:Sprague-Dawley (SD) rats
Dosage:5, 20?mg/kg
Administration:intravenous (i.v.) (5?mg/kg), intraperitoneal (i.p.) (20?mg/kg) and oral (p.o.) (20?mg/kg)
Result:Had good metabolic stability in rats.
体外研究：
RI-962 has potent inhibitory activity for RIPK1 with an IC50 value of 35.0?nM.RI-962 has protective effect for necroptotic death with EC50 values of 10.0 nM, 4.2 nM, 11.4 nM, and 17.8?nM for HT29, L929, J774A.1, and U937 cells, respectively.RI-962 (0-100 μM; 24 h) protectes cells from TSZ-induced necroptosis by inhibiting the kinase activity of RIPK1.
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