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RI-962
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RI-962图片
CAS NO:2763831-53-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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.
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-962i.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 ± 6.3

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.
分子量

480.56

Formula

C28H28N6O2

CAS 号

2763831-53-2

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.