Home Tools

Tranilast

Catalog No. T2690 CAS 53902-12-8

Synonyms: MK 341, SB 252218

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Tranilast, CAS 53902-12-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 36.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 61.00
50 mg	In stock	$ 85.00
100 mg	In stock	$ 122.00
200 mg	In stock	$ 185.00
500 mg	In stock	$ 313.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.57%

Purity: 99.56%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.
Targets&IC50	PGD2:0.1 mM (IC50)
In vitro	In diabetic rats' hearts, Tranilast reduces the phosphorylation of Smad2, effectively mitigating cardiac fibrosis.
In vivo	In hypertrophic and proliferative scar tissues, Tranilast ([3-300 mM]) inhibits collagen synthesis in fibroblasts by suppressing the Transforming Growth Factor (TGF)-β1, yet it does not inhibit the fibroblasts in normal skin.
Kinase Assay	His-tagged human Mps1Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 μg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl2, and 0.5 μg/mL myelin basic protein), AZ3146, and 100 μM γ-[32P]ATP (2 μCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 μM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify 32P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 μM AZ3146[1].

Synonyms	MK 341, SB 252218
Molecular Weight	327.33
Formula	C18H17NO5
CAS No.	53902-12-8

Storage

keep away from direct sunlight,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32.7 mg/mL (100 mM)

References and Literature

1. Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 91-96. 2. Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 85-90. 3. Miyazawa K, et al. Atherosclerosis, 1995, 118(2), 213-221. 4. Martin J, et al. Cardiovasc Res, 2005, 65(3), 694-701. 5. Shiota N, et al. Circulation, 1999, 99(8), 1084-1090. 6. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathway of PI3K/Akt/mTOR in esophageal squamous cell carcinoma[J]. 2020 7. Huang R, Wang F, Yang Y, et al. Recurrent activations of transient receptor potential vanilloid‐1 and vanilloid‐4 promote cellular proliferation and migration in esophageal squamous cell carcinoma cells[J]. FEBS open bio. 2019 Jan 18;9(2):206-225. 8. Liu J, Zhao Z, Wen J, et al. TNF-α differently regulates TRPV2 and TRPV4 channels in human dental pulp cells[J]. International endodontic journal. 2019. 9. Weiqiang H, Longshan Z, Mi Y, et al. Cancer-Associated Fibroblasts Promote the Survival of Irradiated Nasopharyngeal Carcinoma Cells via the NF-κB Pathway[J]. Journal of Experimental & Clinical Cancer Research. 2020

Citations

1. Huang W, Zhang L, Yang M, et al. Cancer-associated fibroblasts promote the survival of irradiated nasopharyngeal carcinoma cells via the NF-κB pathway. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-14 2. Huang W, Zhang L, Yang M, et al. Cancer-associated fibroblasts promote the survival of irradiated nasopharyngeal carcinoma cells via the NF-κB pathway. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-14 3. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathway of PI3K/Akt/mTOR in esophageal squamous cell carcinoma. british journal of cancer. 2022 Nov;127(8):1424-1439. 4. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathways of HSP70/27 and PI3K/Akt/mTOR in esophageal squamous cell carcinoma. British Journal of Cancer. 2022: 1-16. 5. Liu J, Zhao Z, Wen J, et al. TNF-α differently regulates TRPV2 and TRPV4 channels in human dental pulp cells. International endodontic journal. 2019 6. Huang R, Wang F, Yang Y, et al. Recurrent activations of transient receptor potential vanilloid‐1 and vanilloid‐4 promote cellular proliferation and migration in esophageal squamous cell carcinoma cells. FEBS Open Bio. 2019 Jan 18;9(2):206-225 7. Amissah O B, Chen W, de Dieu Habimana J, et al.NY-ESO-1-specific T cell receptor-engineered T cells and Tranilast, a TRPV2 antagonist bivalent treatment enhances the killing of esophageal cancer: a dual-targeted cancer therapeutic route.Cancer Cell International.2024, 24(1): 1-18.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Inhibitor Library GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Traditional Chinese Medicine Monomer Library Drug Repurposing Compound Library Angiogenesis related Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets

Quinapril hydrochloride TRV-120027 TFA Angiotensin II 5-valine TFA Imidapril hydrochloride Eprosartan Losartan Carboxylic Acid Vicenin 2 Vicenin 3

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tranilast 53902-12-8 Endocrinology/Hormones GPCR/G Protein Immunology/Inflammation RAAS Prostaglandin Receptor Inhibitor endothelial chemotaxis tube MK341 anti-atopic prostaglandin SB252218 vascular Angiogenesis SB-252218 Angiotensin Receptor MK-341 proliferation inhibit microvascular MK 341 SB 252218 factor growth inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.