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KI0720Tranilast50 mg$192

Chemical Characteristic

Product NameTranilast
SynonymsRizaben
CAS No.53902-12-8
Molecular Weight 327.34
FormulaC18H17NO5
Chemical Structure

Biological activities

Tranilast is an antiallergic agent. Tranilast inhibits chemical mediator release from mast cells. Tranilast inhibits the proliferation and vascular endothelium growth factor (VEGF)-induced chemotaxis of human dermal microvascular endothelial cells (HDMECs) with IC50 values of 136 and 135 µM , respectively. Tranilast inhibits tube formation of HDMECs cultured on the matrigel as an in vitro angiogenesis model in a concentration-dependent manner.[1] In vitro, tranilast restores cytokine (such as interleukin-1 β, tumor necrosis factor-α, and lipopolysaccharide)-induced nitric oxide production against platelet-derived growth factor in vascular smooth muscle cells.[2] In cultured human skin fibroblasts in vitro, tranilast also inhibits collagen synthesis in a dose-dependent manner to a maximum of 55% at 300 µM during 48 hours of treatment.[3] In vivo angiogenesis in mice, tranilast treatment (0-300 mg/kg) dose-dependently suppresses angiogenesis in the matrigel.[1] In vivo, tranilast also suppresses the content of collagen in granulation tissue of hypersensitive granulomatous inflammation induced by methylated bovine serum albumin (m-BSA) in rats.[4]

Protocols

In vivo: Tranilast is dissolved in 0.5% carboxymethyl cellulose-Na.[1]

References

[1] Isaji M, et al. Tranilast inhibits the proliferation, chemotaxis and tube formation of human microvascular endothelial cells in vitro and angiogenesis in vivo. Br J Pharmacol. 1997, 122(6): 1061-1066.
[2] Hishikawa K, et al. Tranilast restores cytokine-induced nitric oxide production against platelet-derived growth factor in vascular smooth muscle cells. J Cardiovasc Pharmacol. 1996, 28(2): 200-207.
[3] Yamada H, et al. Tranilast, a selective inhibitor of collagen synthesis in human skin fibroblasts. J Biochem. 1994, 116(4): 892-897. 閵嗏偓閵嗏偓
[4] Isaji M, et al. Inhibition by tranilast of collagen accumulation in hypersensitive granulomatous inflammation in vivo and of morphological changes and functions of fibroblasts in vitro. Life Sci. 1994, 55(15): PL287-292. 閵嗏偓閵嗏偓

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