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Muraglitazar

Name: Muraglitazar
Brand: TargetMol
SKU: T21587
Price: 293 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: Pargluva, BMS-298585) Copy Product Info

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Synonyms: Pargluva, BMS-298585

Catalog No. T21587 Copy Product Info

Purity: 99.17%

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Muraglitazar (BMS-298585) is a dual agonist of PPARα/γ that exerts metabolic regulatory effects including lipid modulation, glucose reduction, improvement of insulin resistance, and weight loss. It is indicated for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar exhibits potent in vitro activity against human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM).

Cas No. 331741-94-7

Pack Size	Price	USA Stock	Global Stock
1 mg	$293	In Stock	In Stock
5 mg	$719	In Stock	In Stock
10 mg	$987	In Stock	In Stock
25 mg	$1,490	In Stock	In Stock
50 mg	$1,980	In Stock	In Stock
100 mg	$2,750	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.17%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Muraglitazar AI Summary

Muraglitazar exhibits significant bioactivities, particularly as an agonist of human peroxisome proliferator-activated receptors PPARalpha and PPARgamma. It demonstrates binding affinity with EC50 values of 240.0 nM for PPARalpha and 120.0 nM for PPARgamma in Gal4 transactivation assays. Additionally, it shows inhibition with IC50 values of 250.0 nM for PPARalpha and 190.0 nM for PPARgamma. In animal studies, Muraglitazar has shown to decrease free fatty acid levels, glucose levels, and triglyceride concentrations while increasing insulin levels in male db/db mice, indicating potential antidiabetic effects. The compound also exhibits pharmacokinetic properties such as a half-life of 7.3 hours in male Sprague-Dawley rats after oral administration and a high oral bioavailability of 96.2%. Furthermore, Muraglitazar has displayed an antihyperglycemic effect in db/db mice at dosages as low as 3 mg/kg, significantly reducing blood glucose levels over treatment periods. In in vitro assays, it has shown transactivation of PPARalpha and PPARgamma with Emax values of 84.0% and 128.0%, respectively. These findings suggest Muraglitazar holds considerable potential as a therapeutic agent for conditions related to metabolic dysfunctions, specifically targeting PPARalpha and PPARgamma pathways..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Muraglitazar (BMS-298585) is a dual agonist of PPARα/γ that exerts metabolic regulatory effects including lipid modulation, glucose reduction, improvement of insulin resistance, and weight loss. It is indicated for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar exhibits potent in vitro activity against human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM).
Targets & IC50	PPARα (HEK293 cells):1.41 μM (EC50), PPARα:320 nM (EC50), PPARα:0.42 μM, PPARγ:110 nM (EC50), PPARγ:0.14 μM, PPARγ (HEK293 cells):0.04 μM (EC50)
In vitro	Methods: Steatotic HepaRG cells were treated with 50 μM Muraglitazar for 24 hours or 14 days. After incubation with [¹⁴C]-palmitic acid, β-oxidation products were detected to assess fatty acid oxidation (FAO) activity, and mRNA expression of lipid metabolism and nuclear receptor-related genes was analyzed by RT-qPCR. Results: Short-term treatment with Muraglitazar had no effect on FAO. After 14 days of treatment, Muraglitazar significantly increased FAO activity, downregulated de novo lipogenesis genes, and persistently upregulated FAO-related genes. Additionally, Muraglitazar upregulated the expression of FXR and CAR nuclear receptors, further inhibiting lipid synthesis.[4]
Synonyms	Pargluva, BMS-298585

Chemical Properties

Molecular Weight	516.54
Formula	C₂₉H₂₈N₂O₇
Cas No.	331741-94-7
Smiles	C(COC1=CC=C(CN(C(OC2=CC=C(OC)C=C2)=O)CC(O)=O)C=C1)C=3N=C(OC3C)C4=CC=CC=C4
Relative Density.	1.274g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 128.8 mg/mL (249.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.39 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9360 mL	9.6798 mL	19.3596 mL	96.7979 mL
5 mM	0.3872 mL	1.9360 mL	3.8719 mL	19.3596 mL
10 mM	0.1936 mL	0.9680 mL	1.9360 mL	9.6798 mL
20 mM	0.0968 mL	0.4840 mL	0.9680 mL	4.8399 mL
50 mM	0.0387 mL	0.1936 mL	0.3872 mL	1.9360 mL
100 mM	0.0194 mL	0.0968 mL	0.1936 mL	0.9680 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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