2112809-98-8
中文名稱
JC-171
(JC171)
英文名稱
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 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
密度1.401±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 250 mg/mL (649.64 mM)
酸度系數(shù)(pKa)6.43±0.69(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
JC-171 是選擇性的 NLRP3 炎癥小體抑制劑，抑制 LPS/ATP 誘導(dǎo)的巨噬細(xì)胞釋放 IL-1β 的 IC50 值為 8.45 μM。體外研究
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. |
體內(nèi)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. |