规格

价格

库存

数量

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

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-1:0.8 nM (Ki), Caspase-4:< 0.6 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	贝尔纳卡桑, VX-765

化学信息

分子量	508.99
分子式	C₂₄H₃₃ClN₄O₆
CAS No.	273404-37-8
Smiles	C([C@@H](NC(=O)C1=CC(Cl)=C(N)C=C1)C(C)(C)C)(=O)N2[C@H](C(N[C@@H]3[C@H](OCC)OC(=O)C3)=O)CCC2
密度	1.32 g/cm3

储存&溶解度

存储

溶解度信息

Ethanol: 93 mg/mL (182.71 mM), Sonication is recommended.

DMSO: 240 mg/mL (471.52 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9.3 mg/mL (18.27 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9647 mL	9.8234 mL	19.6468 mL	98.2338 mL
5 mM	0.3929 mL	1.9647 mL	3.9294 mL	19.6468 mL
10 mM	0.1965 mL	0.9823 mL	1.9647 mL	9.8234 mL
20 mM	0.0982 mL	0.4912 mL	0.9823 mL	4.9117 mL
50 mM	0.0393 mL	0.1965 mL	0.3929 mL	1.9647 mL
100 mM	0.0196 mL	0.0982 mL	0.1965 mL	0.9823 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Belnacasan

Belnacasan

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

Belnacasan

Belnacasan

Belnacasan 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词