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J30-8
产品别名
2366255-71-0
J30-8
2-((2-Chlorophenyl)imino)-5-((Z)-5-fluoro-2-oxoindolin-3-ylidene)thiazolidin-4-one
(5Z)-2-(2-Chlorophenylimino)-5-(5-fluoro-2-oxoindolin-3-ylidene)thiazolidin-4-one
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C17H9ClFN3O2S |
Molecular weight | 373.79 |
MDL number | MFCD05026464 |
Biochem/physiol Actions【生化/生理作用】 | J30-8 is a potent c-Jun N-terminal kinase JNK3 subtype-selective inhibtior (human JNK3 IC50 = 40 nM, JNK1α1 & JNK2α2 IC50 >100 μM) that exhibits excellent kinome-wide selectivity (IC50 >7.7 μM against 398 kinase targets) and neuroprotective efficacy against Aβ25-35 toxicity in SH-SY5Y cultures (1 μM). When compared with the pan-JNK inhibitor SP600125 in the APPswe/PS1dE9 murine AD model in vivo (30 mg/kg ip.), J30-8 offers superior therapeutic efficacy and pharmacokinetic properties with longer retention time (elimination t1/2 = 16.11 vs 1.23 hrs; plasma conc = 41 ng/mL vs 22 ng/mL 24 hr post ip.) and greater brain-permeability (brain/plasma ratio = 0.40 vs. 0.14 8 hr post ip.). |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | 2-8℃ |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |