CS17919
CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC50 of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases.
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- No. CAS: 2379346-41-3
- Fòrmula: C22H20F4N6O2
- Peso molecular:476.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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ASK1 22.52 nM (IC50) |
CS17919 (0.32-10 μM; 72 h) provids potent protection in Palmitic acid-treated LO2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L02 cells stimulated with 50 μM Palmitic acid (HY-N0830)
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Concentration:0.32 μM, 0.63 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Significantly prevented apoptosis at all doses.
CS17919 (50 mg/kg; po; twice daily; for 70 days) alleviates glomerular sclerosis in a DKD model[1].
CS17919 (20 mg/kg; po; twice daily; for 4 weeks) ameliorates liver inflammation and fibrosis in a NASH model[1].
Pharmacokinetic parameters of CS17919 in C57BL/6J following oral administration[1].
| Parameters | 20 mg/kg. p.o. | 50 mg/kg. p.o. |
| AUC0-∞ (h·ng/mL) | 23 113 ± 5898.47 | 58 795 ± 23 199.32 |
| AUC0-t (h·ng/mL) | 23 078 ± 5892.78 | 57 239 ± 20 606.29 |
| Cmax (ng/mL) | 4039 ± 646.90 | 5741 ± 1835 |
| MRT0-∞ (h) | 3.96 ± 0.91 | 6.43 ± 1.44 |
| T1/2 (h) | 2.20 ± 0.74 | 3.50 ± 1.86 |
| Tmax (h) | 1.50 ± 0.87 | 2.00 ± 0 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (6-8 weeks old) bearing unilateral ureteral obstruction model (UUO)[1]
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Dosage:10 mg/kg, 60 mg/kg (0.2% CMC-Na + 0.1% Tween-80)
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Administration:po; twice daily; for 11 days
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Result:Preserved kidney function and showed a non-significant tendency to alleviate kidney fibrosis.
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Animal Model:Male neonatal mice bearing chronic kidney disease (CKD)[1]
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Dosage:50 mg/kg
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Administration:po; twice daily; for 70 days
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Result:Significantly improved serum creatinine and glomerular sclerosis.
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Animal Model:Male C57BL/6J mice (6-8 weeks) bearing non-alcoholic steatohepatitis (NASH)[1]
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Dosage:20 mg/kg
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Administration:po; twice daily; for 4 weeks
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Result:Significantly improved liver inflammation and substantially reduced liver fibrosis.
Chemical Information
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No. CAS 2379346-41-3
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Peso molecular 476.43
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Fòrmula C22H20F4N6O2
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SMILES
CC1=C(C=C(C(F)=C1)C(NC2=NC(C3=NN=CN3[C@@H](C(F)(F)F)C)=CC=C2)=O)NC(C4CC4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CS17919 Related Classifications
HY-163752 Related Classifications
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