Belnacasan

产品编号 T6090Cas号 273404-37-8

别名 VX-765

Belnacasan (VX-765) 是一种 IL 转换酶 (ICE)/caspase-1 抑制剂，是 VRT-043198 的口服生物活性前药。Belnacasan 可以修饰 Caspase-1 的活性位点并导致 Caspase-1 阻断，从而与动物模型中炎症疾病的组织保护相关。

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Belnacasan

产品编号 T6090别名 VX-765Cas号 273404-37-8

规格	价格	库存
1 mg	¥ 276	现货
2 mg	¥ 393	现货
5 mg	¥ 647	现货
10 mg	¥ 898	现货
25 mg	¥ 1,780	现货
50 mg	¥ 2,990	现货
100 mg	¥ 3,850	现货
200 mg	¥ 5,520	现货
1 mL x 10 mM (in DMSO)	¥ 762	现货

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产品介绍

生物活性

产品描述	Belnacasan (VX-765) is an IL-converting enzyme (ICE)/caspase-1 inhibitor and an orally bioactive prodrug of VRT-043198. Belnacasan modifies the active site of caspase-1 and leads to caspase-1 blockade, which has been associated with tissue protection against inflammatory diseases in animal models.
靶点活性	Caspase-4:<0.6 nM(Ki), Caspase-1:0.8 nM(Ki)
体外活性	方法：人 PBMCs 和全血用 LPS 和 Belnacasan 处理 18 h，使用 ELISA 检测细胞因子。结果：Belnacasan 抑制 PBMC 和全血的 IL-1β 释放，IC50 值为 0.67 µM 和 1.9 µM。[1]
体内活性	方法：为测试体内活性，将 Belnacasan (25-200 mg/kg) 灌胃给药给 CD-1 小鼠，1 h 后静脉注射 LPS (2 mg/kg)。结果：Belnacasan 在体内抑制 LPS 诱导的 IL-1β 产生。[1] 方法：为检测抗癫痫活性，将 Belnacasan (12.5-200 mg/kg) 腹腔注射给慢性癫痫 C57BL6 小鼠模型，每天两次，持续四天。结果：Belnacasan 的反复全身给药以剂量依赖的方式显著降低了小鼠的慢性癫痫活动。[2]
激酶实验	Enzyme inhibition is assayed by tracking of the rate of hydrolysis of an appropriate substrate labeled with either p-nitroaniline or aminomethyl coumarin (AMC) as follows: ICE/caspase-1, suc-YVAD-p-nitroanilide; caspase-4, Ac-WEHD-AMC; caspase-6, Ac-VEID-AMC; caspase-3, -7, -8, and -9, Ac-DEVD-AMC; and granzyme B, Ac-IEPD-AMC. Enzymes and substrates are incubated in a reaction buffer [10 mM Tris, pH 7.5, 0.1% (w/v) CHAPS, 1 mM dithiothreitol, and 5% (v/v) DMSO] for 10 min at 37°C. Glycerol is added to the buffer at 8% (v/v) for caspase-3, -6, and -9 and granzyme B to improve stability of enzymes. The rate of substrate hydrolysis is monitored using a fluorometer. Assays for cathepsin B and trypsin are performed[2].
细胞实验	VX-765 is solubilized in DMSO and stored, and then diluted with RPMI 1640 complete medium (DMSO 0.2%) before use[1]. A total of 2×105 cells/well (100 μL cell suspension) is distributed in triplicate in flat-bottom 96-well plates. Either 50 μL of VX-765 (40 μM in RPMI 1640 complete medium containing 0.2% DMSO) or vehicle control is added to appropriate wells. Following a 30-min incubation at 37°C, 50 μL of LPS diluted in RPMI 1640 complete medium is added at final concentrations varying from 0.001 to 10 ng/mL. Cells are returned to a 37°C incubator. At 4 h after LPS addition, 75 μL of supernatant is removed from wells, cleared by centrifugation for 5 min at 1500 rpm, and stored at 4°C until assayed. Cells are returned to a 37°C incubator until 24 h after LPS addition, at which time 100 μL of supernatant is removed, cleared by centrifugation, and stored at 4°C. Supernatants are tested using ELISA kits for IL-1β, IL-6, IL-18, and IL-1α[1].
别名	VX-765