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Submit ReviewVX 765
说明： High affinity and selective caspase-4 and caspase 1/ICE inhibitor; orally bioavailable
别名： Belnacasan
化学名： N-(4-Amino-3-chlorobenzoyl)-3-methyl-L-valyl-N-[(2R,3S)-2-ethoxytetrahydro-5-oxo-3-furanyl]-L-prolinamide
纯度： ≥98% (HPLC)
生物活性 for VX 765
VX 765 is a high affinity and selective caspase-4 and caspase 1/ICE inhibitor (Ki of <0.6 and 0.8 nM, respectively). Prodrug of VRT-043198. Inhibits LPS-induced IL-1β production ~ 60% in collagen-induced arthritis mouse model. Exhibits anticonvulsant effects in mouse model of acute seizures. Anti-inflammatory. Orally bioavailable.
化合物库 for VX 765
VX 765 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for VX 765
| 分子量 | 509 |
| 公式 | C24H33ClN4O6 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 273404-37-8 |
| PubChem ID | 11398092 |
| InChI Key | SJDDOCKBXFJEJB-MOKWFATOSA-N |
| Smiles | CCO[C@@H]1OC(C[C@@H]1NC([C@@H]2CCCN2C([C@H](C(C)(C)C)NC(C3=CC(Cl)=C(C=C3)N)=O)=O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VX 765
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 50.9 | 100 | |
| ethanol | 50.9 | 100 |
制备储备液 for VX 765
以下数据基于产品分子量 509。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.82 mL | 19.65 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.93 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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产品说明书 for VX 765
参考文献 for VX 765
参考文献是支持产品生物活性的出版物。
Wu et al (2019) Coptisine from coptis chinensis blocks NLRP3 inflammasome activation by inhibiting caspase-1. Pharmacol.Res. 147 104348 PMID: 31336157
Wannamaker et al (2007) (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 inh J.Pharmacol.Exp.Ther. 321 509 PMID: 17289835
Stack et al (2005) IL-converting enzyme/caspase-1 inhibitor VX-765 blocks the hypersensitive response to an inflammatory stimulus in monocytes from familial cold autoinflammatory syndrome patients. J.Immunol. 175 2630 PMID: 16081838
Xu et al (2019) Caspase-1 inhibitor exerts brain-protective effects against sepsis-associated encephalopathy and cognitive impairments in a mouse model of sepsis. Brain Behav.Immun. 80 859 PMID: 31145977
Yang et al (2019) NLRP3 inflammasome activation promotes the development of allergic rhinitis via epithelium pyroptosis. Biochem.Biophys.Res.Commun. 522 61 PMID: 31740004
If you know of a relevant reference for VX 765, please let us know.
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关键词: VX 765, VX 765 supplier, VX765, high, affinity, selective, caspase4, caspase1, inhibitors, inhibits, anticonvulsant, anti-inflammatory, orally, bioavailable, IL-converting, enzyme, ICE, Belnacasan, Caspases, 7143, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle and DNA Damage Research Product Guide
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There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.