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Tranilast

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Tranilast Basic information
Tranilast Chemical Properties
  • Melting point:166.2-168.2 °C(lit.)
  • Boiling point:465.23°C (rough estimate)
  • Density 1.3185 (rough estimate)
  • refractive index 1.5100 (estimate)
  • storage temp. 2-8°C
  • solubility DMSO: 18 mg/mL
  • form powder
  • pka3.47±0.36(Predicted)
  • color white to beige
  • Merck 14,9570
  • InChIKeyNZHGWWWHIYHZNX-CSKARUKUSA-N
  • CAS DataBase Reference53902-12-8(CAS DataBase Reference)
Safety Information
  • Hazard Codes Xn
  • Risk Statements 22
  • Safety Statements 26-36
  • WGK Germany 3
  • RTECS DG8731000
  • ToxicityLD50 in male, female mice, male, female rats (mg/kg): 780, 680, 1600, 1100 orally; 410, 385, 405, 395 i.p.; 2630, 2820, 3630, 3060 s.c. (Nakazawa, p 385)
MSDS
Tranilast Usage And Synthesis
  • Chemical PropertiesPale Green Solid
  • Usescoronary vasodilator
  • UsesTranilast 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), 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. 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. 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.[Cayman Chemical]
  • UsesAntiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.
  • DefinitionChEBI: An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.
  • Biological ActivityAntiallergic via inhibition of chemical mediator release from mast cells. Most recently shown to be an effective inhibitor of angiogenesis. Demonstrated to antagonize the effects of angiotensin II on human arteries, possibly by an interaction at the level of the AT 1 receptor.
Tranilast Preparation Products And Raw materials
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