Tranilast
Tranilast is an inhibitor of transient receptor potential vanilloid 2 (TRPV2) channels and PDGFRs; it is also a mast cell stabilizer. Tranilast exhibits anti-allergic, anti-fibrotic, immunomodulatory, anti-angiogenic, anti-metastatic, and anticancer chemotherapeutic activities. In animal models of fibrosis, tranilast inhibits mast cell filtration and decreases levels of α-SMA, collagen I, fibronectin, stem cell factor, and c-kit. In other animal models, this compound decreases allograft rejection and induces T cell anergy by increasing expression of p21 and p51, decreasing levels of IL-2, and stimulating cell cycle arrest. In cellular and animal models of breast cancer, tranilast induces G1/S phase cell cycle arrest, decreases levels of TGF-β1 and endoglin, increases levels of p53 and activation of caspase 3 and PARP, and inhibits cell migration, cell proliferation, and tumor growth. In vitro, tranilast inhibits VEGF- and FGF-induced cell proliferation, migration, and tube formation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18977813
| Cas No. |
53902-12-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C18H17NO5 |
| Formula Wt. |
327.34 |
| Chemical Name |
2-[[3-(3,4-Dimethoxyphenyl)-1-oxo-2-propenyl]- amino]benzoic acid |
| IUPAC Name |
2-[[(E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid |
| Synonym |
Rizaben; N-5 |
| Melting Point |
211-213°C |
| Solubility |
DMSO to 100 mM, ethanol to 2 mg/mL, DMF to 35 mg/mL. |
| Appearance |
Light yellow green crystal powder |
Luo J, Li Y, Yang Y, et al. Role and mechanism of tranilast preventing the progression of tubulointerstilial fibrosis in diabetic kidney diseases. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2013 Dec;38(12):1233-42. PMID: 24384948.
Zaher SS, Coe D, Chai JG, et al. Suppression of the allogeneic response by the anti-allergy drug N-(3,4-dimethoxycinnamonyl) anthranilic acid results from T-cell cycle arrest. Immunology. 2013 Feb;138(2):157-64. PMID: 23121382.
Subramaniam V, Chakrabarti R, Prudhomme GJ, et al. Tranilast inhibits cell proliferation and migration and promotes apoptosis in murine breast cancer. Anticancer Drugs. 2010 Apr;21(4):351-61. PMID: 20145538.
Li Y, Liu FY, Peng YM, et al. Mast cell, a promising therapeutic target in tubulointerstitial fibrosis. Med Hypotheses. 2007;69(1):99-103. PMID: 17257770.
Watanabe S, Matsuda A, Suzuki Y, et al. Inhibitory mechanism of tranilast in human coronary artery smooth muscle cells proliferation, due to blockade of PDGF-BB-receptors. Br J Pharmacol. 2000 May;130(2):307-14. PMID: 10807667.
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. Br J Pharmacol. 1999 May;127(2):537-45. PMID: 10385256.
