Belnacasan
Cat. No.：YN270215
CAS No. ：273404-37-8
| 产品名称: | Belnacasan |
| CAS No.: | 273404-37-8 |
| Chemical Name: | N-(4-amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide |
| Synonyms: | VX-765 |
| 分子量: | 509.00 |
| 分子式: | C₂₄H₃₃ClN₄O₆ |
| SMILES: | ClC1=C(N)C=CC(C(N[C@@H](C(C)(C)C)C(N2[C@H](C(N[C@H]3CC(O[C@H]3OCC)=O)=O)CCC2)=O)=O)=C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Belnacasan (VX-765) 是 VRT-043198 的口服生物活性前药，VRT-043198 是有效选择性的 IL 转换酶(ICE)/caspase-1抑制剂，对 caspase-1 的Ki值为 0.8 nM，对 caspase-4 的Ki值小于 0.6 nM。Belnacasan (VX-765) 作用于外周血单核细胞，可抑制 LPS 诱导的 IL-1β 和 IL-18 释放，IC50约为 0.7 μM。 |
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Wannamaker, W., Davies, R., Namchuk, M., et al.(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 (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1β and IL-18J. Pharmacol. Exp. Ther.321(2),509-516(2007)
Maroso, M., Balosso, S., Rivizza, T., et al.Interleukin-1β biosynthesis inhibition reduces acute seizures and drug resistant chronic epileptic activity in miceNeurotherapeutics8(2),304-315(2011)
