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About This Item
Empirical Formula (Hill Notation):
C18H17NO5
CAS Number:
Molecular Weight:
327.33
UNSPSC Code:
41106500
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
Tranilast, ≥98% (HPLC), powder
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
mp
166.2-168.2 °C (lit.)
solubility
DMSO: >10 mg/mL, H2O: insoluble
originator
Kissei
storage temp.
2-8°C
SMILES string
COc1ccc(\C=C\C(=O)Nc2ccccc2C(O)=O)cc1OC
InChI
1S/C18H17NO5/c1-23-15-9-7-12(11-16(15)24-2)8-10-17(20)19-14-6-4-3-5-13(14)18(21)22/h3-11H,1-2H3,(H,19,20)(H,21,22)/b10-8+
InChI key
NZHGWWWHIYHZNX-CSKARUKUSA-N
Gene Information
human ... VEGFA(7422), VEGFB(7423), VEGFC(7424)
Application
The effect of Tranilast on mast cell surface receptors was studied in murine bone marrow-derived mast cells.
Biochem/physiol Actions
Tranilast is an anti-asthma drug, which inhibits LTC4 and PGE2 formation in stimulated monocytes, but does not inhibit cyclooxygenase or lipoxygenase activity; inhibits mast cell degranulation; inhibits VEGF-induced angiogenesis in vivo and also inhibits proliferation and tube formation of human endothelial cells in vitro. Tranilast may represent a new class of drugs for therapy to treat ongoing TH1-mediated autoimmune diseases.
Tranilast is an anti-asthma drug, which inhibits LTC4 and PGE2 formation in stimulated monocytes, inhibits mast cell degranulation, and inhibits VEGF-induced angiogenesis in vivo and also inhibits proliferation and tube formation of human endothelial cells in vitro.
Tranilast also inhibits vascular smooth muscle cell proliferation by inhibiting the cyclin-dependent kinase inhibitor-1(p21Waf1/Cip1) and may be useful in treating cardiac allograft vasculopathy. It is used in treating hypertrophic scars and keloids. Tranilast inhibits tumor necrosis factor (TNF-α and TGF-β2), obstructing epithelial-mesenchymal transition in human retinal pigment epithelial cell line (ARPE).
Features and Benefits
This compound was developed by Kissei. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
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signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Tranilast inhibits the expression of genes related to epithelial-mesenchymal transition and angiogenesis in neurofibromin-deficient cells
Harigai R, et al.
Scientific reports, 8(1), 6069-6069 (2018)
Noriaki Minami et al.
Cancer medicine, 6(11), 2635-2645 (2017-10-06)
Therapeutic options for malignant brain tumors are limited, with new drugs being continuously evaluated. Organotypic brain slice culture has been adopted for neuroscience studies as a system that preserves brain architecture, cellular function, and the vascular network. However, the suitability
Natsuko Kageyama-Yahara et al.
FEBS letters, 584(1), 111-118 (2009-11-12)
Mast cell activation by immunoglobulin E (IgE)-mediated stimuli is a central event in the pathogenesis of allergic disorders. The present report shows that treatment with pentagalloylglucose (PGG) resulted in a down-regulation of FcepsilonRI surface expression on mucosal-type murine bone marrow-derived
