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编 号：F755880
分子式：C23H20N2O6
分子量：420.41
分子式：C23H20N2O6
分子量：420.41
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CAS No: 2768650-56-0
产品详情
生物活性：
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM).
体内研究：
NLRP3-IN-8 (compound 27) (DSS-induced C57BL/6 male mice; 0-20 mg/kg; intragastric; once a day, 7 days) effectively alleviates the severity of DSS-induced colitis in mouse.Animal Model:DSS-induced acute colitis model in C57BL/6 male mice.
Dosage:20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
Administration:Intragastric administration, once a day, 7 days.
Result:Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells.
体外研究：
NLRP3-IN-8 (compound 27) exhibits prominent anti-inflammatory activity with an IC50 of 1.23 μM.NLRP3-IN-8 exhibits good metabolic stability through human liver microsomes (t1/2 = 138.63 min).NLRP3-IN-8 (0-10 μM, 1 h) significantly inhibits pyrolysis rate in a concentration-dependent manner.NLRP3-IN-8 only inhibits the activation of NLRP3 inflammasomes, and could inhibit the activation of inflammasome by a variety of inducer.NLRP3-IN-8 blocks NLRP3-induced ASC oligomerization.NLRP3-IN-8 inhibits NLRP3 inflammasome assembly by blocking the interaction of NLRP3-NEK7 and NLRP3-ASC.
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM).
体内研究：
NLRP3-IN-8 (compound 27) (DSS-induced C57BL/6 male mice; 0-20 mg/kg; intragastric; once a day, 7 days) effectively alleviates the severity of DSS-induced colitis in mouse.Animal Model:DSS-induced acute colitis model in C57BL/6 male mice.
Dosage:20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
Administration:Intragastric administration, once a day, 7 days.
Result:Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells.
体外研究：
NLRP3-IN-8 (compound 27) exhibits prominent anti-inflammatory activity with an IC50 of 1.23 μM.NLRP3-IN-8 exhibits good metabolic stability through human liver microsomes (t1/2 = 138.63 min).NLRP3-IN-8 (0-10 μM, 1 h) significantly inhibits pyrolysis rate in a concentration-dependent manner.NLRP3-IN-8 only inhibits the activation of NLRP3 inflammasomes, and could inhibit the activation of inflammasome by a variety of inducer.NLRP3-IN-8 blocks NLRP3-induced ASC oligomerization.NLRP3-IN-8 inhibits NLRP3 inflammasome assembly by blocking the interaction of NLRP3-NEK7 and NLRP3-ASC.
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