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1. (s)-1-((s)-2-1((-(4-amino-3-chloro-phenyl)-methanoyl)-amino)-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic Acid ((2r,3s)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide
2. (s)-3-((1-((s)-1-((s)-2-((1-(4-amino-3-chlorophenyl)methanoyl)amino)-3,3-dimethyl-butanoyl)pyrrolidin-2yl)methanoyl)amino)-4-oxo-butyric Acid
3. 1-((2s)-2-((4-amino-3-chlorobenzoyl)amino)-3,3-dimethylbutanoyl)-n-((2r,3s)-2- Ethoxy-5-oxo-tetrahydrofuran-3-yl)-l-prolinamide
4. L-prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-l-valyl-n-((1s)-2-carboxy-1-formylethyl)-
5. N-(4-amino-3-chlorobenzoyl)-3-methyl-l-valyl-n-((1s)-2-carboxy-1-formylethyl)-l-prolinamide
6. O-desethyl-belnacasan
7. Vrt 043198
8. Vrt-043198
9. Vx 765
10. Vx-765
11. Vx-765 Hemiketal
12. Vx765
1. Vx-765
2. 273404-37-8
3. Vx765
4. Belnacasan (vx-765)
5. Belnacasan [usan]
6. Belnacasan (vx765)
7. Belnacasan (usan)
8. (s)-1-((s)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-n-((2r,3s)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide
9. 851091-96-8
10. Unii-00ole78529
11. Belnacasan(vx-765)
12. Vx-765 (belnacasan)
13. (2s)-1-[(2s)-2-[(4-amino-3-chlorobenzoyl)amino]-3,3-dimethylbutanoyl]-n-[(2r,3s)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide
14. 00ole78529
15. (2s)-1-[(2s)-2-[(4-amino-3-chlorophenyl)formamido]-3,3-dimethylbutanoyl]-n-[(2r,3s)-2-ethoxy-5-oxooxolan-3-yl]pyrrolidine-2-carboxamide
16. 1-((2s)-2-((4-amino-3-chlorobenzoyl)amino)-3,3-dimethylbutanoyl)-n-((2r,3s)-2- Ethoxy-5-oxo-tetrahydrofuran-3-yl)-l-prolinamide
17. L-prolinamide, N-(4-amino-3-chlorobenzoyl)-3-methyl-l-valyl-n-((2r,3s)-2-ethoxytetrahydro-5-oxo-3-furanyl)-
18. N-(4-amino-3-chlorobenzoyl)-3-methyl-l-valyl-n-[(2r,3s)-2-ethoxytetrahydro-5-oxo-3-furanyl]-l-prolinamide
19. Vx 765
20. Belnacasan [usan:inn]
21. Belnacasan [inn]
22. Belnacasan [who-dd]
23. Gtpl9035
24. Schembl3393597
25. Chembl2107819
26. Chebi:188567
27. Dtxsid901017651
28. Hms3884b11
29. Amy24224
30. Zinc3963010
31. Mfcd11100350
32. S2228
33. Akos024464751
34. Ccg-269769
35. Ncgc00183682-09
36. Ncgc00183682-10
37. Ncgc00183682-13
38. (s)-1-((s)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic Acid ((2r,3s)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide
39. As-35159
40. Bcp0726000319
41. Ft-0774330
42. V0176
43. D10416
44. A857663
45. J-523035
46. Q27075000
47. (s)-1-((s)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-n-((2r,3s)-2-ethoxy-5-oxo-tetrahydrofuran-3-yl)pyrrolidine-2-carboxamide;vx-765
48. 1-((2s)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-n-((2r,3s)-2-ethoxy-5-oxooxolan-3-yl)-l-prolinamide
Molecular Weight | 509.0 g/mol |
---|---|
Molecular Formula | C24H33ClN4O6 |
XLogP3 | 2.3 |
Hydrogen Bond Donor Count | 3 |
Hydrogen Bond Acceptor Count | 7 |
Rotatable Bond Count | 8 |
Exact Mass | 508.2088625 g/mol |
Monoisotopic Mass | 508.2088625 g/mol |
Topological Polar Surface Area | 140 Ų |
Heavy Atom Count | 35 |
Formal Charge | 0 |
Complexity | 818 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 4 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
Investigated for use/treatment in inflammatory disorders (unspecified) and psoriasis and psoriatic disorders.
VX-765 is an orally-absorbed pro-drug of VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. It has been shown to reduce disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation, suggesting that it may be useful for treatment of inflammatory diseases.
VX-765 is a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. In preclinical trials, VX-765 was efficiently converted to VRT-043198 when administered orally to mice and inhibited LPS-induced cytokine secretion. The result was a blocking of IL-1beta and IL-18 secretion, with out much effect on the release of several other cytokines, including IL-1{alpha}, tumor necrosis factor-{alpha}, IL-6 and IL-8. There was also no demonstrable activity in cellular models of apoptosis and it did not affect the proliferation of activated primary T-cells or T-cell lines.