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Belnacasan

CAS No. : 273404-37-8

MCE 国际站：Belnacasan

产品活性：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 K_i 值为 0.8 nM，对 caspase-4 的 K_i 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。

研究领域：Apoptosis

作用靶点：Caspase

In Vivo: Belnacasan reduces inflammatory response in murine models of inflammatory disease.
Belnacasan (50-200 mg/kg) significantly reduces serum IL-1β levels by as much as 60%. It is noteworthy that the effect of Belnacasan on the release of IL-1β induced by LPS reached a plateau at 100 mg/kg. Belnacasan (25-100 mg/kg × 2) significantly reduces ear edema. Belnacasan also dose-dependently reduces the concentrations of cytokines, chemokines, and inflammatory mediators in the ear biopsy samples.
Belnacasan (25-200 mg/kg) significantly delays the time to seizure onset by 1.5- to twofold (p<0.01), reduces the number of seizures by 40% (p<0.01) and the total time spent in EEG seizure activity by 30 to 50% (p<0.01).

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Peptidomimetic Library | Drug Repurposing Compound Library | Pyroptosis Compound Library | Orally Active Compound Library | Z-VAD(OMe)-FMK | Z-DEVD-FMK | Z-IETD-FMK | Tauroursodeoxycholate Sodium | Emricasan | Ac-DEVD-CHO | Guggulsterone | Wedelolactone | Z-YVAD-FMK | Ginsenoside Rh2 | Terfenadine | Dehydrocorydaline chloride | Crustecdysone | Phenoxodiol | Ac-FLTD-CMK | Asperosaponin VI | BOC-D-FMK | Taurodeoxycholic acid sodium hydrate | 2-HBA | Fenbufen | Arnicolide D | Z-WEHD-FMK | ZYZ-488 | 5,​7,​4'-​Trimethoxyflavone | Chelidonic acid | Paris saponin VII

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