| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Significant immunomodulatory activity is exhibited by trojanlast, which also has the ability to prevent the formation of 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). With an IC50 of 10-40 μM and 2-20 μM, respectively, calatorilast prevents monocytes from producing leukotriene C4 or PGE2 when stimulated by A23187 [3]. Tranilast (10-200 μM) has dose-dependent antiproliferative effects in MCF-7 and MDA-MB-231 cell lines. In vitro, tamoxifen (1–20 μM) can also be enhanced in its anti-tumor activity on human breast cancer cells by trenilast (10–200 μM) [4]. HDMEC proliferation is inhibited by trenilast (12.5, 25, 50, and 100 μg/mL; 72 hours) [5].
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|---|---|
| ln Vivo |
In mice, tranilast (300 mg/kg; orally administered twice daily for three days) suppresses angiogenesis in a dose-dependent manner [5].
|
| Cell Assay |
Cell proliferation assay [4]
Cell Types: MCF-7 and MDA-MB-231 Cell Tested Concentrations: 10, 20, 50, 100 and 200 μM Incubation Duration: 48 hrs (hours) Experimental Results: In both cell lines. Cell proliferation assay [5] Cell Types: Human dermal microvascular endothelial cells (HDMEC) Tested Concentrations: 12.5, 25, 50, 100 μg/mL Incubation Duration: 72 hrs (hours) Experimental Results: IC50 value is 44.3 μg/mL (136 μM). |
| Animal Protocol |
Animal/Disease Models: Nineweeks old male C57BL/6 mice [5]
Doses: 300 mg/kg Route of Administration: Orally administered twice a day for 3 days Experimental Results: Inhibition of angiogenesis induced by VEGF in Matrigel; at 300 mg/kg A significant inhibition of 58% was observed at the dose. The ED50 value and 95% confidence limit are 165mg/kg and 162±169mg/kg respectively. |
| References |
[1]. K Ikai , et al. Inhibitory Effect of Tranilast on Prostaglandin D Synthetase. Biochem Pharmacol. 1989 Aug 15;38(16):2673-6.
[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. [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. [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. [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. |
| Molecular Formula |
CL-.NA+
|
|---|---|
| Molecular Weight |
58.4428
|
| CAS # |
104931-56-8
|
| Related CAS # |
trans-Tranilast;70806-55-2;Tranilast;53902-12-8
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=C([O-])C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O.[Na+]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 17.1116 mL | 85.5578 mL | 171.1157 mL | |
| 5 mM | 3.4223 mL | 17.1116 mL | 34.2231 mL | |
| 10 mM | 1.7112 mL | 8.5558 mL | 17.1116 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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