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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.50%
- No. CAS: 2763831-53-2
- Fòrmula: C28H28N6O2
- Peso molecular:480.56
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
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. Further protocols information, click here.
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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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No. CAS 2763831-53-2
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Appearance Solid
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Peso molecular 480.56
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
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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