RI-962
Based on 1 Customer Validation
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.
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- Purity : 99.50%
- CAS No.: 2763831-53-2
- 화학식: C28H28N6O2
- 분자량:480.56
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-29 | EC50 |
10 nM
Compound: RI-962
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Protection against TSZ-induced necroptosis in human HT-29 cells preincubated with compound followed by TNA-alpha,Smac mimetic and Z-VAD-FMK addition and measured after 24 hrs by CCK-8 assay
Protection against TSZ-induced necroptosis in human HT-29 cells preincubated with compound followed by TNA-alpha,Smac mimetic and Z-VAD-FMK addition and measured after 24 hrs by CCK-8 assay
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[PMID: 38159286] |
In Vitro
RI-962 has potent inhibitory activity for RIPK1 with an IC50 value of 35.0 nM[1].
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[1].
RI-962 (0-100 μM; 24 h) protectes cells from TSZ-induced necroptosis by inhibiting the kinase activity of RIPK1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29, L929, J774A.1, and U937 cells
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Concentration:0-100 μM
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Incubation Time:24 h
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Result:Exerted a dose-dependent protective effect against necroptotic death.
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Cell Line:HT29 cells
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Concentration:0-400 nM
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Incubation Time:
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Result:Markedly inhibited the phosphorylation of RIPK1 and its downstream signaling proteins RIPK3 and MLKL in a dose-dependent manner.
In Vivo
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal for 15 min; once a day for 10 day
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Result:Ameliorated TNFα-induced SIRS by inhibiting RIPK1 activity.
Suppressed the RIPK1 signaling in the mouse model of DSS-induced colitis.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:5, 20 mg/kg
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Administration:intravenous (i.v.) (5 mg/kg), intraperitoneal (i.p.) (20 mg/kg) and oral (p.o.) (20 mg/kg)
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Result:Had good metabolic stability in rats.
Chemical Information
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CAS No. 2763831-53-2
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Appearance Solid
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분자량 480.56
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화학식 C28H28N6O2
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Color Off-white to light yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (208.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0809 mL | 10.4045 mL | 20.8091 mL | 52.0226 mL |
| 5 mM | 0.4162 mL | 2.0809 mL | 4.1618 mL | 10.4045 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0809 mL | 5.2023 mL | |
| 15 mM | 0.1387 mL | 0.6936 mL | 1.3873 mL | 3.4682 mL | |
| 20 mM | 0.1040 mL | 0.5202 mL | 1.0405 mL | 2.6011 mL | |
| 25 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0809 mL | |
| 30 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7341 mL | |
| 40 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3006 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL | |
| 100 mM | 0.0208 mL | 0.1040 mL | 0.2081 mL | 0.5202 mL |
RI-962 Related Classifications
HY-148382 Related Classifications
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