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编 号:F020864
分子式:C18H16NNaO5
分子量:349.31
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生物活性:
Tranilast sodium (MK-341 sodium) 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) dose-dependently suppresses angiogenesis in mice.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 exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC50=~1-20 μM), thromboxane B2 (IC50=~10-50 μM), (TGF-β1; IC50=~100-200 μM), and IL-8 (IC50=~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC50s of 10-40 μM and 2-20 μM, respectively.Tranilast (10-200 μM) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cell lines. Tranilast also (10-200μM) enhances the anti-tumor effects of Tamoxifen (1-20 μM) on human breast cancer cells in vitro.Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs.
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