首页 工具
登录
购物车
Belnacasan

Belnacasan

产品编号 T6090   CAS 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。

TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
Belnacasan Chemical Structure
Belnacasan, CAS 273404-37-8
规格 价格/CNY 货期 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 * 10 mM (in DMSO) ¥ 762 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Belnacasan (T6090)
点击图片重新获取验证码
选择批次  
纯度: 99.5%
纯度: 98.45%
纯度: 98.44%
纯度: 97.43%
纯度: 96.53%
TargetMol batch loading
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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 VX-765
分子量 508.99
分子式 C24H33ClN4O6
CAS No. 273404-37-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 93 mg/mL (182.7 mM)

DMSO: 45 mg/mL (88.41 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.9647 mL 9.8234 mL 19.6468 mL 49.1169 mL
5 mM 0.3929 mL 1.9647 mL 3.9294 mL 9.8234 mL
10 mM 0.1965 mL 0.9823 mL 1.9647 mL 4.9117 mL
20 mM 0.0982 mL 0.4912 mL 0.9823 mL 2.4558 mL
50 mM 0.0393 mL 0.1965 mL 0.3929 mL 0.9823 mL
Ethanol 100 mM 0.0196 mL 0.0982 mL 0.1965 mL 0.4912 mL

TargetMol Calculator计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

TargetMol Library Books参考文献

1. Wannamaker W, 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-1beta and IL-18. J Pharmacol Exp Ther. 2007 May;321(2):509-16. 2. Maroso M, et al. Interleukin-1β biosynthesis inhibition reduces acute seizures and drug resistant chronic epileptic activity in mice. Neurotherapeutics. 2011 Apr;8(2):304-15. 3. Maroso M, et al. Neurotherapeutics. 2011, 8(2), 304-315. 4. Akin D, et al. Neurobiol Dis. 2011, 44(3), 259-269. 5. Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer[J]. MLA . Cancers. 2020, 12(1): 194.

TargetMol Library Books文献引用

1. Zhao Q, Feng H, Yang Z, et al. The central role of a two‐way positive feedback pathway in molecular targeted therapies‐mediated pyroptosis in anaplastic thyroid cancer. Clinical and Translational Medicine. 2022, 12(2): e727 2. Zhao Q, Feng H, Yang Z, et al. The central role of a two‐way positive feedback pathway in molecular targeted therapies‐mediated pyroptosis in anaplastic thyroid cancer. Clinical and Translational Medicine. 2022, 12(2): e727 3. Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer MLA. Cancers. 2020, 12(1): 193. 4. Hussain M, Lu Y, Tariq M, et al. A small-molecule Skp1 inhibitor elicits cell death by p53-dependent mechanism. Iscience. 2022, 25(7): 104591. 5. Xia H, Zhang Z, You F. Inhibiting ACSL1-Related Ferroptosis Restrains Murine Coronavirus Infection. Viruses. 2021, 13(12): 2383. 6. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 7. Liu M, Wang Y, Li S, et al.Attenuates reactive oxygen species: induced pyroptosis via activation of the Nrf2/HO-1 signal pathway in models of trigeminal neuralgia.Scientific Reports.2023, 13(1): 18111. 8. Liu Z, Dang B, Li Z, et al.Baicalin attenuates acute skin damage induced by ultraviolet B via inhibiting pyroptosis.Journal of Photochemistry and Photobiology B: Biology.2024: 112937.
Phenoxodiol Pomolic acid δ-secretase inhibitor 11 Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone 5,7-Dihydroxychromone Isolimonexic acid Jolkinolide B Altholactone

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抑制剂库 抗癌临床化合物库 药物功能重定位化合物库 抗衰老化合物库 抗癌化合物库 人代谢物化合物库 细胞凋亡化合物库 临床期小分子药物库 细胞焦亡化合物库

TargetMol Calculator剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

TargetMol Calculator 体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Belnacasan 273404-37-8 Apoptosis Proteases/Proteasome Caspase Inhibitor VX 765 VX765 inhibit VX-765 inhibitor

 

TargetMol Loading
陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼