Art. -Nr.: HY-B0195

Tranilast

(Synonyms: MK-341; SB 252218)

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC₅₀= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells.

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Reinheit: 99.95%
CAS. Nr.: 53902-12-8
Formel: C₁₈H₁₇NO₅
Molecular Weight:327.33

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Tranilast Chemical Structure

CAS. Nr.: 53902-12-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC₅₀= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects^[1]. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells^[2].

IC₅₀ & Target

Angiotensin II

DP2

0.1 mM (IC₅₀)

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen :

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	126 μM Compound: 11	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy	[PMID: 30878828]
L02	IC₅₀	82.3 μM Compound: 1; TR	Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36037790]
RBL-2H3	IC₅₀	0.49 mM Compound: Tranilast	Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay	[PMID: 12398545]
RBL-2H3	IC₅₀	0.49 mM Compound: Tranilast	Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins	[PMID: 15387643]

In Vitro

Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC₅₀=~1-20 μM), thromboxane B2 (IC₅₀=~10-50 μM), (TGF-β1; IC₅₀=~100-200 μM), and IL-8 (IC₅₀=~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC₅₀s of 10-40 μM and 2-20 μM, respectively^[3].
Tranilast (10-200 μM) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cell lines. Tranilast also (10-200μM) enhances the anti-tumor effects of Tamoxifen (1-20 μM) on human breast cancer cells in vitro^[4].
Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:

MCF-7 and MDA-MB-231 cells
Concentration:

10, 20, 50, 100, and 200 μM
Incubation Time:

48 hours
Result:

Anti-proliferative effect in a dose-dependent manner in both cell lines.

Cell Viability Assay^[5]

Cell Line:

Human dermal microvascular endothelial cells (HDMECs)
Concentration:

12.5, 25, 50, 100 μg/mL
Incubation Time:

72 hours
Result:

IC₅₀ value was 44.3 μg/mL (136 μM).

In Vivo

Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nine-week-old male C57BL/6 mice^[5]
Dosage:

300 mg/kg
Administration:

Administered orally twice a day for 3 days
Result:

Suppressed the VEGF-induced angiogenesis in matrigel; 58% of significant suppression was observed at a dose of 300 mg/kg.
The ED₅₀ value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.

Chemical Information

CAS. Nr. 53902-12-8
Appearance Solid
Molecular Weight 327.33
Formel C₁₈H₁₇NO₅
Color Light yellow to green yellow
SMILES

O=C(O)C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O
Synonyms

MK-341; SB 252218
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (9)

All Bio/Physico-chemical AssayCell Imaging/StainingWBIHC

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Journal Impact Factor

Cell Metab

Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]

2022 Mar 1;34(3):424-440.e7. PMID: 35150639
Autophagy

Cannabidiol inhibits human glioma by induction of lethal mitophagy through activating TRPV4. [Abstract]

2021 Nov;17(11):3592-3606. PMID: 33629929
Mol Cell

Cytosolic DNA sensing by cGAS/STING promotes TRPV2-mediated Ca2+ release to protect stressed replication forks. [Abstract]

2023 Jan 14;S1097-2765(22)01217-5. PMID: 36696898

Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]

Tranilast treatment (50 μM) on HU-induced [Ca²⁺]_i elevation in S phase-synchronized HeLa cells treated with HU (2 mM, 4 h).

Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]

Tranilast treatment (50 μM) on the ER release of Ca²⁺ in S phase-synchronized HeLa cells treated with HU (2 mM, 4 h).

Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]

Effects of Tranilast treatment (50 μM) on T172-phosphorylation of AMPKα in HeLa cells treated with HU (2 mM, 4 h). γH2AX IF signal marks the cells with replication stress.

Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]

Effects of Tranilast treatment (50 μM) on S746-phosphorylation of Exo1-GFP in HeLa cells treated with HU (2 mM) for 4 h.

Tranilast purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]

Effects of Tranilast on [Ca²⁺]_i. in HeLa cells transfected with ssDNA or dsDNA fragments (2 μg/ml). Cells were imaged 6 h after transfection and Tranilast (50 μM) or DMSO was added 4 h before imaging.
Cell Death Differ

ALKBH5 aggravates scarring after glaucoma surgery via m6A-YTHDF2-mediated NLRP3 mRNA stabilization. [Abstract]

2026 May 31. PMID: 42218253
Mol Biomed

ML345 is a potent and selective NLRP3 inflammasome inhibitor with anti-inflammatory activity. [Abstract]

2025 Nov 13;6(1):108. PMID: 41231359
Cell Death Dis

TGF-β1-mediated downregulation of L1CAM in pancreatic ductal adenocarcinoma drives upregulation of collagen 17A1 and MMP2, facilitating tumor invasiveness and metastasis. [Abstract]

2025 Aug 6;16(1):592. PMID: 40770187
Pharmacol Res

Sinomenine-induced histamine release-like anaphylactoid reactions are blocked by tranilast via inhibiting NF-κB signaling. [Abstract]

2017 Nov;125(Pt B):150-160. PMID: 28867637

Tranilast purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2017 Nov;125(Pt B):150-160. [Abstract]

The IL-33 production in different treatment groups is determined in rat skin by immunohistochemistry assay.
Cell Calcium

TRPV2 inhibitor tranilast prevents atrial fibrillation in rat models of pulmonary hypertension. [Abstract]

2024 Jan:117:102840. PMID: 38160478
J Interferon Cytokine Res

Effects of Tranilast on Inflammasome and Macrophage Phenotype in a Mouse Model of Myocardial Infarction. [Abstract]

2021 Mar;41(3):102-110. PMID: 33750216

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (152.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0550 mL

15.2751 mL

30.5502 mL

5 mM

0.6110 mL

3.0550 mL

6.1100 mL

10 mM

0.3055 mL

1.5275 mL

3.0550 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (7.64 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 30% SBE-β-CD in Saline

Solubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 1.5% CMC-Na/saline water

Solubility: 4 mg/mL (12.22 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. K Ikai , et al. Inhibitory Effect of Tranilast on Prostaglandin D Synthetase. Biochem Pharmacol. 1989 Aug 15;38(16):2673-6. [Content Brief]

[2]. K Miyazawa , et al. Tranilast Antagonizes Angiotensin II and Inhibits Its Biological Effects in Vascular Smooth Muscle Cells. Atherosclerosis. 1996 Apr 5;121(2):167-73. [Content Brief]

[3]. E A Capper, et al. Modulation of Human Monocyte Activities by Tranilast, SB 252218, a Compound Demonstrating Efficacy in Restenosis. J Pharmacol Exp Ther. 2000 Dec;295(3):1061-9. [Content Brief]

[4]. Sara Darakhshan, et al. Tranilast Enhances the Anti-Tumor Effects of Tamoxifen on Human Breast Cancer Cells in Vitro. J Biomed Sci. 2013 Oct 21;20(1):76. [Content Brief]

[5]. M Isaji , et al. Tranilast Inhibits the Proliferation, Chemotaxis and Tube Formation of Human Microvascular Endothelial Cells in Vitro and Angiogenesis in Vivo. Br J Pharmacol. 1997 Nov;122(6):1061-6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0550 mL	15.2751 mL	30.5502 mL	76.3755 mL
	5 mM	0.6110 mL	3.0550 mL	6.1100 mL	15.2751 mL
	10 mM	0.3055 mL	1.5275 mL	3.0550 mL	7.6376 mL
	15 mM	0.2037 mL	1.0183 mL	2.0367 mL	5.0917 mL
	20 mM	0.1528 mL	0.7638 mL	1.5275 mL	3.8188 mL
	25 mM	0.1222 mL	0.6110 mL	1.2220 mL	3.0550 mL
	30 mM	0.1018 mL	0.5092 mL	1.0183 mL	2.5459 mL
	40 mM	0.0764 mL	0.3819 mL	0.7638 mL	1.9094 mL
	50 mM	0.0611 mL	0.3055 mL	0.6110 mL	1.5275 mL
	60 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2729 mL
	80 mM	0.0382 mL	0.1909 mL	0.3819 mL	0.9547 mL
	100 mM	0.0306 mL	0.1528 mL	0.3055 mL	0.7638 mL

Tranilast

9 Cited Publications

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Tranilast

GPCR/G Protein Compound Library

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Anti-Prostate Cancer Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

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Cysteine Targeted Covalent Library

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Multi-Target Compound Library

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MCE Bioactive Compound Library

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FDA-Approved Drug Library Plus

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Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Tranilast

Alle Angiotensin Receptor Isoform-spezifische Produkte anzeigen

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tranilast Related Classifications

HY-B0195 Related Classifications