Belnacasan (VX-765)
目录号：S2228
Molecular Weight(MW): 509
Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。
客户使用该产品的5个实验数据：
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(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
Cell, 2018, 175(2):442-457. Belnacasan (VX-765) purchased from Selleck.
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BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control.
Mucosal Immunol, 2015, 10.1038/mi.2015.44. Belnacasan (VX-765) purchased from Selleck.
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(c,d) HMDMs and BMMs were treated as above for 1 h. Cell lysates, as well as cell culture supernatants, were analyzed by western blot for cleavage of caspase-1. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as loading control. Similar results were obtained in two independent experiments. Ctrl, control; DMSO, dimethyl sulfoxide.
Mucosal Immunol, 2016, 9(1):124-36. Belnacasan (VX-765) purchased from Selleck.
(A) LPS-primed J774A.1 macrophages were treated with DCA (100 μM) in the presence or absence of caspase-1 inhibitor belnacasan (10 μM). IL-1β in supernatants was analyzed by ELISA.
Front Immunol, 2016, 7:536.. Belnacasan (VX-765) purchased from Selleck.
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(A, B and C) Quantitative real‐time PCR for the transcript expression levels of matrix metalloproteinases 3, matrix metalloproteinases 13 and COL2A1 in NP cells after treatment with AGEs‐BSA (100 μg/ml) or recombinant human IL‐1β (1 ng/ml) for 48 hrs, combined with si‐NLRP3, VX‐765 and IL‐1Ra or not. Data were presented as mean ± S.D. (n = 3). *P < 0.05 versus control, #P < 0.05 versus AGEs‐BSA + si‐control, &P < 0.05 versus IL‐1β.
J Cell Mol Med, 2017, 21(7):1373-1387. Belnacasan (VX-765) purchased from Selleck.
产品安全说明书
Caspase抑制剂选择性比较
生物活性
| 产品描述 | Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。 | ||||
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| 特性 | 一种有效的选择性白介素-转化酶/半胱天冬酶-1抑制剂。 | ||||
| 靶点 |
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| 体外研究 |
VX-765是一种口服可吸收的VRT-043198前药，其对ICE/caspase-1 和caspase-4表现出有效的抑制作用，Ki 分别为0.8 nM 和<0.6 nM。VRT-043198也会抑制IL-1β从PBMCs和全血中的释放，IC50分别为0.67 μM 和1.9 μM。[1] |
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| 体内研究 | 在胶原诱导的关节炎小鼠模型中，VX-765 (200 mg/kg)抑制60% LPS诱导的IL-1β产生，并导致炎症比例剂量依赖性显著减少，对关节病变也能够产生有效保护作用。[1]在体内，VX-765通过防止前脑星形胶质细胞中IL-1β的增加阻断大鼠体内的癫痫发生，而对后放电持续时间没有显著影响。[2]在急性癫痫小鼠模型中，VX-765 (50 mg/kg-200 mg/kg)通过延迟首次癫痫开始时间，并减少平均50%的癫痫发作次数以及64%的总持续时间，产生抗痉挛作用。[3]在患有遗传性失神癫痫的成年大鼠体内，VX-765药物注射3天后，通过选择性阻断IL-1β生物合成，显著降低累积持续时间和平均55%的棘慢波放电(SWDs)。[4] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 动物实验：[1] |
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溶解度 (25°C)
| 体外 | DMSO | 100 mg/mL warmed (196.46 mM) |
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| Ethanol | 100 mg/mL warmed (196.46 mM) | |
| Water | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 509 |
|---|---|
| 化学式 | C24H33ClN4O6 |
| CAS号 | 273404-37-8 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01501383 | Terminated | Epilepsy | Vertex Pharmaceuticals Incorporated | December 2011 | Phase 2 |
| NCT01501383 | Terminated | Epilepsy | Vertex Pharmaceuticals Incorporated | December 2011 | Phase 2 |
| NCT01048255 | Completed | Partial Epilepsy | Vertex Pharmaceuticals Incorporated | January 2010 | Phase 2 |
| NCT01048255 | Completed | Partial Epilepsy | Vertex Pharmaceuticals Incorporated | January 2010 | Phase 2 |
| NCT00205465 | Completed | Psoriasis | Vertex Pharmaceuticals Incorporated | December 2004 | Phase 2 |
| NCT00205465 | Completed | Psoriasis | Vertex Pharmaceuticals Incorporated | December 2004 | Phase 2 |
技术支持
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如果有其他问题，请给我们留言。
常见问题及建议解决方法
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问题 1：
The recommended dose of VX-765 is 100mg/kg p.o. in 25% cremophor EL in water. Is VX0765 directly soluble at 10mg/ml in 25% cremophor in water? How to formulate it for in vivo use in mice?
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回答：
You can prepare 25% cremophor EL in water first and then directly resuspend VX-765 powder in the vehicle. The powder may not be fully dissolved, but the suspension is stable and can be used for gavage feeding.
