| Identification | Back Directory | [Name]
Benzamide, 5-[(cyclopropylcarbonyl)amino]-2-fluoro-4-methyl-N-[6-[4-[(1R)-2,2,2-trifluoro-1-methylethyl]-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- | [CAS]
2379346-41-3 | [Synonyms]
Benzamide, 5-[(cyclopropylcarbonyl)amino]-2-fluoro-4-methyl-N-[6-[4-[(1R)-2,2,2-trifluoro-1-methylethyl]-4H-1,2,4-triazol-3-yl]-2-pyridinyl]- | [Molecular Formula]
C22H20F4N6O2 | [MOL File]
2379346-41-3.mol | [Molecular Weight]
476.43 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
CS17919 (10-60 mg/kg; po; twice daily; for 11 days) improves kidney injury and fibrosis in the UUO model[1].
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].
1.19 | 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 |
| Animal Model: | Male C57BL/6J mice (6-8?weeks old) bearing unilateral ureteral obstruction model (UUO)[1] | | Dosage: | 10?mg/kg, 60?mg/kg (0.2% CMC-Na?+?0.1% Tween-80) | | Administration: | po; twice daily; for 11?days | | Result: | Preserved kidney function and showed a non-significant tendency to alleviate kidney fibrosis. |
| Animal Model: | Male neonatal mice bearing chronic kidney disease (CKD)[1] | | Dosage: | 50?mg/kg | | Administration: | po; twice daily; for 70?days | | Result: | Significantly improved serum creatinine and glomerular sclerosis. |
| Animal Model: | Male C57BL/6J mice (6-8?weeks) bearing non-alcoholic steatohepatitis (NASH)[1] | | Dosage: | 20?mg/kg | | Administration: | po; twice daily; for 4?weeks | | Result: | Significantly improved liver inflammation and substantially reduced liver fibrosis.
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| [IC 50]
ASK1: 22.52 nM (IC50) | [References]
[1] Guoqiang Liao, et al. Targeting ASK1 by CS17919 alleviates kidney- and liver-related diseases in murine models. Animal Model Exp Med. 2024 Jun 14. DOI:10.1002/ame2.12437 |
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