PGD 2 0.1 mM (IC 50 ) Angiotensin II

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 ED 50 value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.

Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC 50 =~1-20 μM), thromboxane B2 (IC 50 =~10-50 μM), (TGF-β1; IC 50 =~100-200 μM), and IL-8 (IC 50 =~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC 50 s 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. Cell Proliferation Assay Cell Line: MCF-7 and MDA-MB-231 cells Concentration: 10, 20, 50, 100, and 200 μM Incubation Time: 48 hours Result: Anti-proliferative effect in a dose-dependent manner in both cell lines. Cell Proliferation Assay Cell Line: Human dermal microvascular endothelial cells (HDMECs) Concentration: 12.5, 25, 50, 100 μg/mL Incubation Time: 72 hours Result: IC 50 value was 44.3 μg/mL (136 μM).

Tranilast sodium (MK-341 sodium) 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。