产品
编 号:F386793
分子式:C4H7NO2S
分子量:133.17
产品类型
10mM*1mL in DMSO
440
In-stock
结构图
CAS No: 54863-37-5
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生物活性:
Dapansutrile is a potent, orally active and selective NLRP3 inflammasome inhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases.
体内研究:
Dapansutrile (3.75 g/kg;口服;每日一次,连续 22 天) 改善实验性自身免疫性脑脊髓炎 (EAE) 小鼠的神经衰退和神经组织损伤。Dapansutrile (3.75 g/kg;口服 每日一次,连续 22 天) 降低实验性自身免疫性脑脊髓炎 (EAE) 小鼠脊髓中促炎细胞因子的蛋白质水平。Dapansutrile (6-600 mg/kg;腹腔注射;一次;雄性 ICR (CD1) 小鼠) 减少梗塞面积并降低心脏中的 caspase-1 活性。Dapansutrile (6-600 mg/kg;腹腔注射;一次,持续 24 小时和 7 天;急性心肌梗死小鼠) 在心肌缺血再灌注损伤后保持心脏功能。Animal Model:EAE-induced female adult C57BL/6 (8–10 weeks old)
Dosage:3.75 g/kg
Administration:Oral administration; daily, for 22 days
Result:Ameliorated the neurological deficits of EAE disease.Reduced the levels of IL-1β, L-18 , TNFα, CXCL-1 and IL-6. Showed ~2-fold reduction in the infiltration of T cells (CD45+, CD3+). Reduced the accumulation macrophages (CD45high, CD11b+, F4/80+), microglia (CD45low, CD11b+), and other cells (CD45+, CD11b-, CD3-, CD24+).
Animal Model:Male ICR (CD1) mice (8-12 weeks old)
Dosage:6, 60, and 600 mg/kg
Administration:Intraperitoneal injection; once
Result:Reduced infarct size in a dose-dependent manner.
Animal Model:Mice subjected to acute myocardial infarction (AMI)
Dosage:6, 60, and 600 mg/kg
Administration:Intraperitoneal injection; once, for 24 hours and 7 days
Result:Preserved left ventricular (LV) systolic function at 24 hours.Increased in cardiac function at 7 days of reperfusion when compared with the control mice.