产品
编 号:F383649
分子式:C18H17NO5
分子量:327.33
产品类型
结构图
CAS No: 53902-12-8
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产品详情
生物活性:
Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC50= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells.
体内研究:
Tranilast (300 mg/kg; administered orally twice a day for 3 days) 剂量依赖性地抑制小鼠的血管生成。Animal Model:Nine-week-old male C57BL/6 mice
Dosage:300 mg/kg
Administration:Administered orally twice a day for 3 days
Result:Suppressed the VEGF-induced angiogenesis in matrigel; 58% of significant suppression was observed at a dose of 300 mg/kg. The ED50 value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.
体外研究:
Tranilast 表现出显著的免疫调节活性,可抑制内毒素诱导的前列腺素 E2 (PGE2; IC50=~1-20 μM)、血栓素 B2 (IC50=~10-50 μM),(TGF-β1;IC50=~100-200 μM),和 IL-8 (IC50=~100 μM) 形成。Tranilast 抑制 A23187 诱导的单核细胞白三烯 C4 或 PGE2 形成,IC50 分别为 10-40 μM 和 2 -20 μM。 Tranilast (10 -200 μM) 在 MCF-7 和 MDA-MB-231 细胞系中表现出剂量依赖性的抗增殖作用。Tranilast (10 -200 μM) 还增强他莫昔芬 (1 -20 μM) 在体外对人乳腺癌细胞的抗肿瘤作用。 Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) 抑制 HDMECs 的增殖。