Tranilast
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.95%
- CAS No.: 53902-12-8
- 화학식: C18H17NO5
- 분자량:327.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tranilast
More- Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
- Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
- Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5. [Abstract]
- Cell Death Differ. 2026 May 31. [Abstract]
- Mol Biomed. 2025 Nov 13;6(1):108. [Abstract]
- Cell Death Dis. 2025 Aug 6;16(1):592. [Abstract]
- Pharmacol Res. 2017 Nov;125(Pt B):150-160. [Abstract]
- Cell Calcium. 2024 Jan:117:102840. [Abstract]
- J Interferon Cytokine Res. 2021 Mar;41(3):102-110. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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WB
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Bio/Physico-chemical Assay
All Angiotensin Receptor Isoforms
More
Biological Activity
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Angiotensin II |
DP2 0.1 mM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
126 μM
Compound: 11
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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
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[PMID: 30878828] |
| L02 | IC50 |
82.3 μM
Compound: 1; TR
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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
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[PMID: 36037790] |
| RBL-2H3 | IC50 |
0.49 mM
Compound: Tranilast
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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
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[PMID: 12398545] |
| RBL-2H3 | IC50 |
0.49 mM
Compound: Tranilast
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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
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[PMID: 15387643] |
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.
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Cell Line:MCF-7 and MDA-MB-231 cells
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Concentration:10, 20, 50, 100, and 200 μM
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Incubation Time:48 hours
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Result:Anti-proliferative effect in a dose-dependent manner in both cell lines.
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Cell Line:Human dermal microvascular endothelial cells (HDMECs)
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Concentration:12.5, 25, 50, 100 μg/mL
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Incubation Time:72 hours
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Result:IC50 value was 44.3 μg/mL (136 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nine-week-old male C57BL/6 mice[5]
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Dosage:300 mg/kg
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Administration:Administered orally twice a day for 3 days
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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
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CAS No. 53902-12-8
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Appearance Solid
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분자량 327.33
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화학식 C18H17NO5
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Color Light yellow to green yellow
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SMILES
O=C(O)C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O
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Synonyms
MK-341; SB 252218
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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