RI-962 是一种有效的选择性受体相互作用蛋白激酶 1(RIPK1)抑制剂。RI-962 抑制 RIPK1，IC50值为 35.0 nM。RI-962 可用于神经系统疾病和炎症性疾病的研究。
| 生物活性 | RI-962 is a potent and selectivereceptor-interacting protein kinase 1 (RIPK1)inhibitor. RI-962 inhibitsRIPK1with anIC50value of 35.0 nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases[1]. |
| IC50& Target | IC50: 35.0 nM (RIPK1); EC50: 10.0 nM (HT29 cells), 4.2 nM (L929 cells), 11.4 nM (J774A.1 cells), 17.8 nM (U937 cells)[1]. |
体外研究
(In Vitro) | RI-962 has potent inhibitory activity for RIPK1 with an IC50value of 35.0 nM[1].
RI-962 has protective effect for necroptotic death with EC50values of 10.0 nM, 4.2 nM, 11.4 nM, and 17.8 nM for HT29, L929, J774A.1, and U937 cells, respectively[1].
RI-962 (0-100 μM; 24 h) protectes cells from TSZ-induced necroptosis by inhibiting the kinase activity of RIPK1[1].
Cell Viability Assay[1] | Cell Line: | HT29, L929, J774A.1, and U937 cells | | Concentration: | 0-100 μM | | Incubation Time: | 24 h | | Result: | Exerted a dose-dependent protective effect against necroptotic death. |
Western Blot Analysis[1] | Cell Line: | HT29 cells | | Concentration: | 0-400 nM | | Incubation Time: | | | Result: | Markedly inhibited the phosphorylation of RIPK1 and its downstream signaling proteins RIPK3 and MLKL in a dose-dependent manner. |
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体内研究
(In Vivo) | 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[1].
Pharmacokinetic Parameters of RI-962 in rats (i.v., i.p., p.o.; 5, 20 mg/kg)[1].
| RI-962 | i.v. | p.o. | i.p. | | Dose (mg/kg) | 5 | 20 | 20 | | T1/2(h) | 2.1 ± 0.2 | 1.3 ± 0.2 | 8.5 ± 1.6 | | Tmax(h) | 0.1 ± 0.0 | 0.8 ± 1.0 | 0.5 ± 0.0 | | Cmax(ng/mL) | 12170.4 ± 1198.5 | 674.2 ± 424.7 | 3603.3 ± 693.3 | | AUC0–t(ng*h/mL) | 4526.1 ± 546.0 | 1594.9 ± 891.8 | 6459.7 ± 1131.6 | | AUC0–∞(ng*h/mL) | 4538.1 ± 546.3 | 1604.5 ± 896.1 | 6609.3 ± 1121.4 | | Vss(L/kg) | 0.4 ± 0.1 | - | - | | MRT0–∞(h) | 0.4 ± 0.0 | 1.8 ± 0.2 | 2.8 ± 0.1 | | CL (mL/min/kg) | 18.5 ± 2.1 | - | - | | F (%) | - | 8.8 ± 5.0 | 35.7 ± 6.3 |
| Animal Model: | C57BL/6 female mice[1] | | 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[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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