JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages.
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 MOG35–55-specific Th17 cells in the spleens and spinal cords of EAE mice.
分子式
C16H17ClN2O5S
分子量
384.83
CAS号
2112809-98-8
运输条件
Room temperature in continental US; may vary elsewhere.