104931-56-8
104931-56-8 用途与合成方法
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PGD 2 0.1 mM (IC 50 ) |
Angiotensin II
|
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 (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. |
