| 货号 | 13044-5mg |
| 描述 | Tranilast is a compound that exhibits anti-inflammatory and immunomodulatory effects by inhibiting lipid mediator and cytokine release from inflammatory cells and interfering with PDGF- and TGF-β1-induced proliferation and migration of vascular medial smooth muscle cells. Tranilast suppresses production of prostaglandin D2(IC50 = 0.1 mM)1, prostaglandin E2(IC50 = ~1-20 µM), thromboxane B2(IC50 = ~10-50 µM), TGF-β1 (IC50 = ~100-200 µM), and interleukin-8 (IC50 = ~100 µM) in in vitro models as well as attenuates of the proinflammatory activity of human monocytes.2 While originally marketed as an antiallergenic drug, the efficacy of tranilast in preventing restenosis after percutaneous coronary intervention has been tested in a large-scale clinical trial.3 Additionally, tranilast inhibits VEGF-induced angiogenetic activities (i.e., proliferation, migration and tube formation of vascular endothelial cells) with IC50 values of 22, 18 and 193 µM, which may prove therapeutic for various retinal diseases.4 |
| 别名 | N-(3,4-Dimethyoxycinnamoyl) Anthranilic Acid;MK 341;Rizaben;SB 252218;Tranpro; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ikai, K.,Ujihara, M.,Fujii, K., et al. Inhibitory effect of tranilast on prostaglandin D synthetase. Biochemical Pharmacology 38(16), 2673-2676 (1989). 2.Capper, E.A.,Roshak, A.K.,Bolognese, B.J., et al. Modulation of human monocyte activities by tranilast, SB 252218, a compund demonstrating efficacy in restenosis. Journal of Pharmacology and Experimental Therapeutics 295(3), 1061-1069 (2000). 3.Holmes, D.R., Jr.,Savage, M.,LaBlanche, J.M., et al. Results of prevention of restenosis with tranilast and its outcomes (PRESTO) trial. Circulation 106, 1243-1250 (2002). 4.Koyama, S.,Takagi, H.,Otani, A., et al. Tranilast inhibits protein kinase C-dependent signalling pathway linked to angiogenic activities and gene expression of retinal microcapillary endothelial cells. British Journal of Pharmacology 127, 537-545 (1999). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 327.3 |
| 分子式 | C18H17NO5 |
| CAS号 | 53902-12-8 |
| 稳定性 | ≥ 2 years |
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