Identification | Back Directory | [Name]
Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- | [CAS]
1383420-08-3 | [Synonyms]
CRV431 Rencofilstat Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- | [Molecular Formula]
C67H122N12O13 | [MOL File]
1383420-08-3.mol | [Molecular Weight]
1303.76 |
Chemical Properties | Back Directory | [Boiling point ]
1362.6±65.0 °C(Predicted) | [density ]
1.017±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.33±0.70(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
Rencofilstat (CRV431) is a pan-cyclophilin inhibitor with IC50 values of 2.5 nM, 3.1 nM, 2.8 nM, 7.3 nM for Cyp A, CypB, Cyp D and Cyp G, respectively. Rencofilstat reduces fibrosis and tumor growth in models of chronic liver disease[1]. | [in vivo]
Rencofilstat (50 mg/kg, po, daily for 8 weeks) exhibits anti-fibtosis and antitumor activities in the mouse nonalcoholic steatohepatitis (NASH) model[1]. Animal Model: | Mouse nonalcoholic steatohepatitis (NASH) model[1] | Dosage: | 50 mg/kg | Administration: | po, daily for 8 weeks | Result: | Decreased liver fibrosis, reduced the number and size of liver tumors. |
| [IC 50]
Cyclophilin A: 2.5 nM (IC50); Cyclophilin B: 3.1 nM (IC50); Cyclophilin D: 2.8 nM (IC50); Cyclophilin G: 7.3 nM (IC50) | [References]
[1] Joseph Kuo, et al. A Pan-Cyclophilin Inhibitor, CRV431, Decreases Fibrosis and Tumor Development in Chronic Liver Disease Models. J Pharmacol Exp Ther. 2019 Nov;371(2):231-241. |
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