[CAS NO. 2763831-53-2] RI-962
PRODUCTS SPECIFICATIONS [2763831-53-2]
DESCRIPTION [2763831-53-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 480.56 |
| Molecular Formula | C28H28N6O2 |
| SMILES | O=C(C1=CN(C)C2=C1C=C(C3=CC4=NC(NC(C(C)C)=O)=NN4C=C3)C=C2)NC(C)C5=CC=CC=C5 |
Summary
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] .
In Vitro
RI-962 has potent inhibitory activity for RIPK1 with an IC
50
value of 35.0 nM
[1]
.
RI-962 has protective effect for necroptotic death with EC
50
values 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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 |
| T 1/2 (h) | 2.1 ± 0.2 | 1.3 ± 0.2 | 8.5 ± 1.6 |
| T max (h) | 0.1 ± 0.0 | 0.8 ± 1.0 | 0.5 ± 0.0 |
| C max (ng/mL) | 12170.4 ± 1198.5 | 674.2 ± 424.7 | 3603.3 ± 693.3 |
| AUC 0–t (ng*h/mL) | 4526.1 ± 546.0 | 1594.9 ± 891.8 | 6459.7 ± 1131.6 |
| AUC 0–∞ (ng*h/mL) | 4538.1 ± 546.3 | 1604.5 ± 896.1 | 6609.3 ± 1121.4 |
| V ss (L/kg) | 0.4 ± 0.1 | - | - |
| MRT 0–∞ (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 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.