VX-765
- Belnacasan
- Optical Purity: 0.99
- Soluble in DMSO
- MF: C24H33ClN4O6
- MW: 509
Description
VX-765 is a novel Caspase-1 inhibitor being investigated for the treatment of epilepsy, currently being developed by Vertex. VX-765 is an orally-absorbed pro-drug of VRT-043198, a potent and selective inhibitor of ICE/caspase-1 sub-family caspases. VRT-043198 exhibits 100-10,000-fold selectivity against other caspase-3 and -6-9. In cultures of peripheral blood mononuclear cells and whole blood from healthy subjects stimulated with bacterial products, VRT-043198 inhibited the release of Interleukin (IL)-1beta and IL-18, but had little effect on the release of several other cytokines, including IL-1alpha, tumor necrosis factor-alpha, IL-6 and IL-8.
More Information
| Parent CAS No. | 273404-37-8 |
|---|---|
| Chemical Name | (S)-1-((S)-2-(4-Amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C(C(N[C@@H](C(C)(C)C)C(=O)N2CCC[C@H]2C(N[C@H]2CC(=O)O[C@H]2OCC)=O)=O)C=C(Cl)C=1N |&1:5,16,19,24,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H33ClN4O6/c1-5-34-23-16(12-18(30)35-23)27-21(32)17-7-6-10-29(17)22(33)19(24(2,3)4)28-20(31)13-8-9-15(26)14(25)11-13/h8-9,11,16-17,19,23H,5-7,10,12,26H2,1-4H3,(H,27,32)(H,28,31)/t16-,17-,19+,23+/m0/s1 |
| InChiKey | SJDDOCKBXFJEJB-MOKWFATOSA-N |
| CID | 11398092 |
| Short Description | Caspase-1 inhibitor |
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