Art. -Nr.: HY-17445

Muraglitazar

(Synonyms: BMS-298585)

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Muraglitazar (BMS-298585) is an orally active non-thiazolidinedione oxybenzylglycine dual-target PPARα/PPARγ agonist, with an IC₅₀ of 0.25 μM and an EC₅₀ of 0.32 μM against human PPARα, and an IC₅₀ of 0.19 μM and an EC₅₀ of 0.11 μM against human PPARγ. Muraglitazar regulates lipid homeostasis, enhances peripheral insulin sensitivity, and improves β-cell function. Muraglitazar reduces levels of blood glucose, insulin, triglycerides and free fatty acids, normalizes adiponectin and corticosterone levels, promotes cholesterol efflux, reduces hepatic lipid content, regulates body weight, prevents hyperglycemia, and improves glucose tolerance. Muraglitazar can be used in research related to type 2 diabetes and dyslipidemia.

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Reinheit: 98.38%
CAS. Nr.: 331741-94-7
Formel: C₂₉H₂₈N₂O₇
Molecular Weight:516.54

Speicherung:

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

Muraglitazar Chemical Structure

CAS. Nr.: 331741-94-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

hPPARα

0.25 μM (IC₅₀)

hPPARγ

0.19 μM (EC₅₀)

hPPARα

0.32 μM (IC₅₀)

hPPARγ

0.11 μM (EC₅₀)

Alle PPAR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.035 μM Compound: I	Agonist activity at GAL4 tagged human PPARgamma ligand binding domain expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at GAL4 tagged human PPARgamma ligand binding domain expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25686852]
HEK293	EC₅₀	0.04 μM Compound: 1, muraglitazar	Agonist activity at human PPARgamma expressed in HEK293 cells assessed as luciferase activity by GAL4 transactivation assay Agonist activity at human PPARgamma expressed in HEK293 cells assessed as luciferase activity by GAL4 transactivation assay	[PMID: 18511276]
HEK293	EC₅₀	1.41 μM Compound: 1, muraglitazar	Agonist activity at human PPARalpha expressed in HEK293 cells assessed as luciferase activity by GAL4 transactivation assay Agonist activity at human PPARalpha expressed in HEK293 cells assessed as luciferase activity by GAL4 transactivation assay	[PMID: 18511276]
HEK293	EC₅₀	1.41 μM Compound: I	Agonist activity at GAL4 tagged human PPARalpha ligand binding domain expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at GAL4 tagged human PPARalpha ligand binding domain expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25686852]
HepG2	EC₅₀	0.09 μM Compound: muraglitazar	Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells	[PMID: 18976908]
HepG2	EC₅₀	0.15 μM Compound: muraglitazar	Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells	[PMID: 18976908]

In Vitro

Muraglitazar (1.0 μM) induces potent PPARγ-mediated differentiation of 3T3L-1 preadipocytes, resulting in triglyceride accumulation comparable to the selective PPARγ agonist rosiglitazone^[1].
Muraglitazar (10 µM) increases reverse cholesterol transport gene expression and stimulates 78% cholesterol efflux in differentiating THP1 macrophage cells^[2].

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

Parmacokinetics

Species	Dose	Route	T_max	C_max	Bioavailability	AUC_0-∞
Rat^[1]	10.0 mg/kg	p.o.	0.4 h	20.8 μg/mL	88 %	49.0 μg·h/mL
Dog^[1]	1 mg/kg	p.o.	0.6 h	0.12 μg/mL	18 %	/
Cynomolgus Monkey^[1]	2 mg/kg	p.o.	0.6 h	15.7 μg/mL	79 %	/

In Vivo

Muraglitazar (10 mg/kg; p.o.; once daily; for 14 consecutive days) significantly reduces plasma glucose levels by 54%, triglyceride levels by 33%, free fatty acid levels by 62%, and insulin levels by 48% in male db/db mice^[1].
Muraglitazar (0.1-30 mg/kg; p.o.; daily; 2-4 weeks) produces dose-dependent, persistent improvements in blood glucose, blood lipid and hormone parameters in severely diabetic db/db mice, with the dose of 10 mg/kg/day reducing fasting blood glucose by 51% within 2 weeks^[2].
Muraglitazar (1-10 mg/kg; p.o.; daily; 12 weeks) reduces the risk of hyperglycemia in prediabetic db/db mice by up to 72%, and restores the pancreatic insulin content of mice to normal within 12 weeks^[2].
Muraglitazar (10 mg/kg; p.o.; daily) reduces hepatic triglyceride content by 39% and decreases cholesterol content by up to 63% in mice and hamsters with diabetes complicated by hyperlipidemia induced by a high-fat diet^[2].

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

Animal Model:

db/db (male)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Reduced plasma glucose by 54%.
Reduced triglycerides by 33%.
Reduced free fatty acids by 62%.
Reduced insulin by 48%.

Animal Model:

db/db (severely diabetic)^[2]
Dosage:

10 mg/kg/day (2-week treatment); 0.1-30 mg/kg/day (4-week treatment); ≥1 mg/kg/day (4-week treatment)
Administration:

p.o.; daily; 2 weeks or 4 weeks
Result:

Reduced fasting glucose by 51% and postoral glucose by 30%.
Dose-dependently reduced plasma triglycerides, free fatty acids, glucose, and insulin.
Normalized abnormally low plasma adiponectin and elevated corticosterone levels.
Reduced urine output from 12 mL to 1.9 mL.
Produced sustained glucose lowering.
Normalized adiponectin levels to lean mouse levels.
Increased both fat mass and lean mass without altering bone mineral content.
Did not increase food consumption.

Animal Model:

db/db (prediabetic, normoglycemic, 5-week-old)^[2]
Dosage:

1 mg/kg/day; 3 mg/kg/day; 10 mg/kg/day
Administration:

p.o.; daily; 12 weeks
Result:

Prevented the onset of hyperglycemia by 51-72%.
Reduced glycosylated hemoglobin by 34-55%.
Reduced insulin levels by 23-54% and C-peptide levels by 19-51%.
Improved glucose tolerance.
Normalized pancreatic insulin content to lean mouse levels.

Animal Model:

high-fat diet-induced diabetic/hyperlipidemic^[2]
Dosage:

10 mg/kg/day
Administration:

p.o.; daily
Result:

Reduced liver triglyceride content by 39% and cholesterol content by 49% in mice.
Reduced liver triglyceride content by 39% and cholesterol content by 63% in hamsters.
Did not increase liver weight.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 331741-94-7
Appearance Solid
Molecular Weight 516.54
Formel C₂₉H₂₈N₂O₇
Color White to off-white
SMILES

O=C(O)CN(C(OC1=CC=C(OC)C=C1)=O)CC2=CC=C(OCCC3=C(C)OC(C4=CC=CC=C4)=N3)C=C2
Synonyms

BMS-298585
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (96.80 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

1.9360 mL

9.6798 mL

19.3596 mL

5 mM

0.3872 mL

1.9360 mL

3.8719 mL

10 mM

0.1936 mL

0.9680 mL

1.9360 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (4.84 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.84 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.

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 (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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]. Devasthale, Pratik V., et al. "Design and synthesis of N-[(4-Methoxyphenoxy) carbonyl]-N-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl) ethoxy] phenyl] methyl] glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor α/γ dual agonist with efficacious glucose and lipid-lowering activities." Journal of Medicinal Chemistry 48.6 (2005): 2248-2250.

[2]. Cox SL, et al. Muraglitazar: an agent for the treatment of type 2 diabetes and associated dyslipidemia. Drugs of today (Barcelona, Spain : 1998). 2005 Sep;41(9):579-87. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9360 mL	9.6798 mL	19.3596 mL	48.3990 mL
	5 mM	0.3872 mL	1.9360 mL	3.8719 mL	9.6798 mL
	10 mM	0.1936 mL	0.9680 mL	1.9360 mL	4.8399 mL
	15 mM	0.1291 mL	0.6453 mL	1.2906 mL	3.2266 mL
	20 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4199 mL
	25 mM	0.0774 mL	0.3872 mL	0.7744 mL	1.9360 mL
	30 mM	0.0645 mL	0.3227 mL	0.6453 mL	1.6133 mL
	40 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2100 mL
	50 mM	0.0387 mL	0.1936 mL	0.3872 mL	0.9680 mL
	60 mM	0.0323 mL	0.1613 mL	0.3227 mL	0.8066 mL
	80 mM	0.0242 mL	0.1210 mL	0.2420 mL	0.6050 mL

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Muraglitazar

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Mitochondrial Toxicity Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Muraglitazar

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Mitochondrial Toxicity Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Muraglitazar Related Classifications

HY-17445 Related Classifications