JC-171 (JC171)
| 中文名称 | JC-171 (JC171) |
|---|---|
| 中文同义词 | |
| 英文名称 | JC-171 (JC171) |
| 英文同义词 | JC-171 (JC171);Benzamide, 5-chloro-N-[2-[4-[(hydroxyamino)sulfonyl]phenyl]ethyl]-2-methoxy- |
| CAS号 | 2112809-98-8 |
| 分子式 | C16H17ClN2O5S |
| 分子量 | 384.83 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2112809-98-8.mol |
| 结构式 |  |
JC-171 (JC171) 性质
| 密度 | 1.401±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：250 mg/ml（649.64 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 6.43±0.69(Predicted) |
| 颜色 | 白色至米白色 |
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。
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. |
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. |