RIPK1-IN-41
RIPK1-IN-41 is an orally active RIPK1 inhibitor with an IC50 of 92 nM and a KD of 106.8 nM. RIPK1-IN-41 reduces the phosphorylation level of RIPK1, inhibits necrosome formation, blocks the activation of RIPK3 and MLKL, maintains mitochondrial and lysosomal functions, preserves cell membrane integrity, and suppresses necroptosis. RIPK1-IN-41 alleviates hypothermia and multi-organ damage in a mouse model of systemic inflammatory response syndrome induced by mTNF-α. RIPK1-IN-41 is applicable to research related to systemic inflammatory response syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H33N5O2
- Molecular Weight:471.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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RIPK1 92 nM (IC50) |
RIPK1 106.8 nM (Kd) |
RIPK1-IN-41 (Compound 5e) potently inhibits purified RIPK1 kinase with an IC50 of 92 nM[1].
RIPK1-IN-41 directly binds to purified RIPK1 kinase with a K0 of 106.8 nM[1].
RIPK1-IN-41 strongly inhibits purified RIPK1, moderately inhibits purified RIPK3, and retains multi-targeted activity against several other kinases including VEGFR2, PDGFRβ, and FLT3[1].
RIPK1-IN-41 dose-dependently inhibits mTNF-α/Z-VAD-FMK-induced necroptosis in L929 cells with an EC50 of 0.45 μM[1].
RIPK1-IN-41 (0.05-1 μM) can maintain, in a dose-dependent manner, the mitochondrial integrity and lysosomal integrity of mTNF-α/Z-VAD-FMK-induced necrotic apoptosis in L929 cells, inhibit the formation of RIPK1-RIPK3 necrosomes, upregulate pMLKL activation and lysosomal translocation[1].
RIPK1-IN-41 (0.5 μM; 3-6 h) time-dependently inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in mTNF-α/Z-VAD-FMK-induced necroptotic L929 cells[1].
RIPK1-IN-41 (0.05-1 μM,1 h pretreatment; 6 h necroptosis induction) reduced phosphorylation of RIPK1, RIPK3, and MLKL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse L929 fibroblast cells (induced with mTNF-α/Z-VAD-FMK)
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Concentration:0.05, 0.5, 1 μM
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Incubation Time:1 h pretreatment; 6 h necroptosis induction
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Result:Dose-dependently reduced phosphorylation of RIPK1, RIPK3, and MLKL.
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Cell Line:mouse L929 fibroblast cells (induced with mTNF-α/Z-VAD-FMK)
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Concentration:0.5 μM
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Incubation Time:3 h, 6 h
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Result:Time-dependently reduced phosphorylation of RIPK1, RIPK3, and MLKL.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-t | AUC0-∞ |
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| Rat[1] | 10 mg/kg | p.o. | 39.2 ng/mL | 0.89 h | 2.19 h | 183.3 ng·h/mL | 189.6 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[1]
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Dosage:30 mg/kg; 50 mg/kg
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Administration:p.o.; single dose; 1 hour prior to mTNF-α injection
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Result:Achieved a 50% 48-hour survival rate.
Decreased serum IL-6 levels to 627.0 pg/mL from the model group's 1034.2 pg/mL.
Alleviated hypothermia relative to the model group.
Achieved an 83% 48-hour survival rate.
Reached a body temperature nadir of 32.5 °C at 10 hours and recovered to normal levels by 28 hours.
Decreased serum IL-6 levels to 433.9 pg/mL
Significantly reduced damage to heart, liver, spleen, lung, and kidney, with tissue morphology near that of the normal control group.
Chemical Information
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Molecular Weight 471.59
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Formel C28H33N5O2
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SMILES
CCN(CCNC(C1=C(NC(/C=C2C(NC3=CC=C(C=C3\2)C4=CC(N)=CC=C4)=O)=C1C)C)=O)CC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RIPK1-IN-41 Related Classifications
HY-183781 Related Classifications
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