Tranilast
For research use only.
Catalog No.S1439 Synonyms: SB 252218
4 publications
CAS No. 53902-12-8
Tranilast (SB 252218) 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.
Selleck's Tranilast has been cited by 4 publications
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Biological Activity
| Description | Tranilast (SB 252218) 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 |
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 | 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] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 66 mg/mL (201.63 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 327.33 |
|---|---|
| Formula | C18H17NO5 |
| CAS No. | 53902-12-8 |
| Storage |
powder in solvent |
| Synonyms | SB 252218 |
| Smiles | COC1=C(C=C(C=C1)C=CC(=O)NC2=CC=CC=C2C(=O)O)OC |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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