Home Immunology & Inflammation Immunology & Inflammation related chemical Tranilast For research use only.

Tranilast

Synonyms: SB 252218, MK-341

Tranilast is an antiallergic drug by inhibiting lipid mediator and cytokine release from inflammatory cells, used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Tranilast Chemical Structure

Tranilast Chemical Structure

CAS No. 53902-12-8

Purity & Quality Control

Tranilast Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ECs Function assay Evaluated for inhibition of proliferation of human coronary artery endothelial cells (ECs), induced by 5 % FBS., IC50 = 19.1 μM. 11229768
SMCs Function assay Inhibition of human coronary artery smooth muscle cells (SMC's) proliferation, induced by platelet-derived growth factor (PDGF-BB) 20 ng mL., IC50 = 24.5 μM. 11229768
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Biological Activity

Description Tranilast is an antiallergic drug by inhibiting lipid mediator and cytokine release from inflammatory cells, used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.
In vitro
In vitro Tranilast is an anti-allergic drug inhibiting the release of substances such as histamine and prostaglandins from mast cells, which suppresses collagen synthesis of fibroblasts derived from keloid tissues. Tranilast (3-300 mM) suppresses the collagen synthesis of fibroblasts from keloid and hypertrophic scar tissue but not healthy skin fibroblasts. Tranilast (30-300 mM) inhibits the release of transforming growth factor (TGF)-beta 1 from keloid fibroblasts, which enhances the collagen synthesis of keloid fibroblasts. [1] Tranilast improves keloids and hypertrophic scars which originate from the abnormal proliferation and excessive collagen accumulation of fibroblasts. Tranilast inhibits the release of TGF-beta 1, IL-1 beta and PGE2 from the human monocytes-macrophages. [2] Tranilast inhibits the proliferation stimulated with fetal bovine serum (FBS), TGF-beta 1 and platelet-derived growth factor-BB (PDGF-BB) as well as PDGF-BB-induced migration. Tranilast exhibits inhibitory effects on spontaneous collagen synthesis and TGF-beta 1-induced collagen and glycosaminoglycan synthesis. [3]
In Vivo
In vivo Tranilast results in a 58% reduction in TGF-beta1-induced 3[H]-hydroxyproline incorporation in the diabetic heart of rats. Tranilast attenuates cardiac fibrosis by 37% in association with reduction in phospho-Smad2 in the diabetic heart of rats. [4] Tranilast treatment completely prevents the increase in chymaselike activity, reduces the chymase mRNA levels by 43%, and decreases the carotid intima/media ratio by 63% in the carotid artery of dogs. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05626829 Recruiting
Nasopharyngeal Carcinoma|Recurrent Cancer
Jian Guan|Nanfang Hospital Southern Medical University
 July 20 2022 Phase 2
NCT00882024 Completed
Active Rheumatoid Arthritis
Nuon Therapeutics Inc.
 March 2009 Phase 2
NCT01003613 Completed
Pterygium
Gildasio Castello de Almeida Junior|Hospital de Base|Sao Jose do Rio Preto Medical School
 February 2009 Phase 3
NCT00717808 Withdrawn
Rheumatoid Arthritis
Imperial College London|Nuon Therapeutics Inc.
 September 2008 Phase 1

Chemical Information & Solubility

Molecular Weight 327.33 Formula

C18H17NO5
CAS No. 53902-12-8 SDF Download Tranilast SDF
Smiles COC1=C(C=C(C=C1)C=CC(=O)NC2=CC=CC=C2C(=O)O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (198.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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