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Tranilast

Name: Tranilast
Brand: Selleck Chemicals
SKU: S1439
Rating: 5 (13 reviews)

Synonyms: SB 252218, MK-341

Catalog No.S1439 Purity: 99.97%

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

CAS: 53902-12-8

Selleck's Tranilast has been cited by 13 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.97%

99.97

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Cell Data

Cell Lines	Assay Type	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

Handling Instructions

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