Belnacasan NEW
| Price | $31 | $46 | $78 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: Belnacasan | CAS No.: 273404-37-8 |
| Purity: 99.5% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | Belnacasan |
| 描述 | Belnacasan (VX-765) is an orally active inhibitor of IL-converting enzyme/caspase-1. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 激酶實(shí)驗(yàn) | 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]. |
| 體外活性 | VX-765 demonstrates antiepileptic properties by preventing the increase of IL-1β in the forebrain astrocytes of rats, thereby inhibiting the occurrence of epilepsy without significantly affecting the duration of post-discharge. In adult rats with genetic absence epilepsy, a 3-day administration of VX-765 significantly reduces the cumulative duration and decreases the average spike-wave discharges by 55% through the selective blockade of IL-1β biosynthesis. In acute epileptic mouse models, doses ranging from 50 mg/kg to 200 mg/kg of VX-765 delay the onset of the first epileptic episode and reduce the average number of seizures by 50% and the total duration by 64%. Additionally, a 200 mg/kg dose in a collagen-induced arthritis mouse model suppresses 60% of lipopolysaccharide-induced IL-1β production and leads to a dose-dependent significant reduction in inflammation scores, effectively protecting against joint lesions. |
| 體內(nèi)活性 | VRT-043198 inhibits the release of IL-1β from peripheral blood mononuclear cells (PBMCs) and whole blood, with IC50 values of 0.67 μM and 1.9 μM, respectively. VX-765, an orally bioavailable prodrug of VRT-043198, demonstrates potent inhibition of ICE/caspase-1 and caspase-4, with Ki values of 0.8 nM and <0.6 nM, respectively. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 9.3 mg/mL (18.27 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : 93 mg/mL (182.7 mM) DMSO : 45 mg/mL (88.41 mM) |
| 關(guān)鍵字 | Inhibitor | VX 765 | VX765 | Belnacasan | inhibit | Caspase |
| 相關(guān)產(chǎn)品 | Taurodeoxycholic acid | Allethrin | Crustecdysone | SKLB-163 | Fenbufen | Cystamine | Taurochenodeoxycholic Acid | Tauroursodeoxycholate sodium | CIL62 | Tauroursodeoxycholate | Allicin | PAC-1 |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗心血管疾病化合物庫(kù) | 抗衰老化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 抗癌藥物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Henan Aochuang Chemical Co.,Ltd.
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2022-10-13 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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