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Tranilast

CAS No. : 53902-12-8

MCE 国际站：Tranilast

产品活性：Tranilast (MK-341) 是一种抗变态反应剂。抑制前列腺素 D2 产生 (PGD2，IC₅₀=0.1 mM)。具有抗炎和免疫调节作用。Tranilast sodium 拮抗血管紧张素 II (angiotensin II) 并抑制其在血管平滑肌细胞中的生物学作用。

研究领域：GPCR/G Protein

作用靶点：Angiotensin Receptor  |  Prostaglandin Receptor

In Vitro: 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.

In Vivo: Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice.

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