化合物VX-702 T2513

Product Introduction
Bioactivity


英文名: VX-702

描述: VX702 是一种高度特异性的 p38α MAPK 抑制剂，对 p38α 的选择性比 p38β 高 14 倍。它是一种小分子研究口服抗细胞因子疗法，用于治疗炎症性疾病，如类风湿性关节炎。

激酶实验: HDAC enzyme assay in vitro: The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.

体外活性: 每天两次VX-702（0.1 mg/kg）处理与甲胺喋呤（0.1 mg/kg）处理效果接近.此外,每天两次VX-702（5 mg/kg）处理与每天一次氢化泼尼松（10 mg/kg）处理效果类似.与对照组和用5 mg/kg VX-702处理实验组相比,50 mg/kg实验组的MI/AAR比率显著降低.VX-702半衰期为16-20 h,半数清除剂量3.75 L,分布容积为73 L/kg. VX-702对p38 MAPK活性具有选择性抑制作用,但不影响ERKs和JNKs.

体内活性: VX-702不影响p38 MAPK兴奋剂诱导的血小板聚集。用VX-702（1 μM）处理血小板,可完全或部分抑制由血小板兴奋剂(包括凝血酵素,AYPGKF,SFLLRN,U46619和胶原)诱导的p38活性（IC50：4-20 nM）。VX-702剂量依赖性地抑制IL-6（IC50：59 ng/ml）、IL-1β（IC50：122 ng/ml）和TNFα（IC50：99 ng/ml）的产生。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 75 mg/mL (185.5 mM)


关键字: VX-702 | Inhibitor | p38 MAPK | inhibit | VX702 | VX 702 | Autophagy

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相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Liver Cancer Compound Library | Oxidation-Reduction Compound Library | Fluorochemical Library | Osteogenesis Compound Library | Inhibitor Library | Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | MAPK Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途