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2112809-98-8

中文名称 JC-171 (JC171)
英文名称 JC-171 (JC171)
CAS 2112809-98-8
分子式 C16H17ClN2O5S
分子量 384.83
MOL 文件 2112809-98-8.mol
2112809-98-8 结构式 2112809-98-8 结构式

基本信息

英文别名
JC-171 (JC171)
Benzamide, 5-chloro-N-[2-[4-[(hydroxyamino)sulfonyl]phenyl]ethyl]-2-methoxy-

物理化学性质

密度1.401±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 250 mg/mL (649.64 mM)
酸度系数(pKa)6.43±0.69(Predicted)
形态Solid
颜色White to off-white

常见问题列表

生物活性
JC-171 是选择性的 NLRP3 炎症小体抑制剂,抑制 LPS/ATP 诱导的巨噬细胞释放 IL-1β 的 IC50 值为 8.45 μM。
体外研究

JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently.

Cell Viability Assay

Cell Line: J774A.1 murine macrophage cells
Concentration: 0-100 μM.
Incubation Time: 0.5 h (before LPS (1 μg/mL) treatment for 4.5 h).
Result: Inhibited the release of IL-1β in J774A.1 cells upon stimulation with LPS/ATP.
体内研究

JC-171 treatment delays the progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE) in mouse.

Animal Model: Mice immunized subcutaneously with 200 μg Myelin oligodendrocyte glycoprotein (MOG) 35–55 peptide emulsified in Complete Freund’s Adjuvant (CFA) on day 0 followed by injection of 200 ng of pertussis toxin.
Dosage: 100 mg/kg, 10 mg/kg.
Administration: IP days 0, 1 and 2; and every other days thereafter (100 mg/kg).
Initiated when the clinical scores of individual mice have reached 1 (flaccid tail), and given every other day (10 mg/kg).
Result: Efficiently suppressed EAE progression compared with vehicle treatment.
Resulted in a substantial decrease in the frequency of MOG 35–55 -specific Th17 cells in the spleens and spinal cords of EAE mice.
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