Tranilast (Synonyms: MK-341; SB 252218)

Name: Tranilast
Brand: MedChemExpress
SKU: HY-B0195
Rating: 5.0 (8 reviews)

Cat. No.: HY-B0195 Purity: 99.95%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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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CAS No. : 53902-12-8

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 8 publication(s) in Google Scholar

Other Forms of Tranilast:

trans-Tranilast In-stock
Tranilast sodium 견적 받기
Tranilast (Standard) 견적 받기

8 Publications Citing Use of MCE Tranilast

Bio/Physico-chemical Assay

Cell Imaging/Staining

IHC

: 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.

: 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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Biological Activity
순도&문서
References
고객리뷰

제품 설명

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)

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.

분자량

327.33

화학식

C₁₈H₁₇NO₅

CAS No.

53902-12-8

Appearance

Solid

Color

Light yellow to green yellow

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.95%

Select Batch:

Data Sheet (279 KB) SDS (396 KB)

COA (248 KB) HNMR (258 KB) RP-HPLC (247 KB) LCMS (94 KB)

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

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tranilast (Synonyms: MK-341; SB 252218)

고객리뷰

Other Forms of Tranilast:

Tranilast Related Antibodies

8 Publications Citing Use of MCE Tranilast

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Angiotensin Receptor Isoform Specific Products:

View All Prostaglandin Receptor Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Tranilast Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Tranilast Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report