Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)-
- CAS No.
- 1383420-08-3
- Chemical Name:
- Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)-
- Synonyms
- CRV431;Rencofilstat;Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)-
- CBNumber:
- CB58232637
- Molecular Formula:
- C67H122N12O13
- Molecular Weight:
- 1303.76
- MDL Number:
- MOL File:
- 1383420-08-3.mol
Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- Properties
Boiling point | 1362.6±65.0 °C(Predicted) |
---|---|
Density | 1.017±0.06 g/cm3(Predicted) |
pka | 13.33±0.70(Predicted) |
form | Solid |
color | White to off-white |
FDA UNII | M3H4D91AY5 |
Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- Chemical Properties,Uses,Production
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.
Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- Preparation Products And Raw materials
Raw materials
Preparation Products
Cyclosporin A, 6-[(2S,3R,4R)-10-(acetylamino)-3-hydroxy-4-methyl-2-(methylamino)decanoic acid]-8-(N-methyl-D-alanine)- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 20670 | 58 |
Supplier | Advantage |
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TargetMol Chemicals Inc. | 58 |