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Muraglitazar Sale

(Synonyms: 莫格他唑 ,BMS-298585) 目录号 : GC14246

A PPARα and PPARγ dual agonist

Muraglitazar Chemical Structure

Cas No.:331741-94-7

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产品描述

IC50: 0.42 μM: shows agonistic activity at peroxisome proliferator-activated receptor α (PPARα)

IC50: 0.14 μM: shows agonistic activity at PPARγ.

Muraglitazar, a dual agonist of PPARα and PPARγ, induces an increase in HDL-C levels, a reduction of apolipoprotein B, total cholesterol, HbA1c and triglyceride. Muraglitazar is related to an increased risk of heart failure and adverse cardiovascular events. The PPARs, as a subfamily of the 48-member nuclear-receptor superfamily, regulate gene expression in response to ligand binding and are probably involved in pathogenesis, including insulin resistance, diabetes as well as its related complications. PPARα and PPARγ function in adipocyte maturation, lipid metabolism, and fatty acid storage.

In vitro: In murine J774 macrophages, Muraglitazar dose-dependently reduced lipopolysaccharide-induced inducible nitric oxide synthase (iNOS) expression, nitrous oxide, IL-6 and TNFα production and showed no effect on cell viability at the given concentration. Muraglitazar decreased the levels of iNOS mRNA expression, suggesting that the suppressive effect of muraglitazar was mediated at the level of iNOS transcription. In human HEK293 cells, muraglitazar did not affect the nuclear levels of NF- κB p65 compared to the control and did not modulate NF-κB-mediated transcription [1].

In vivo: Male Charles River mice were administrated orally with muraglitazar at a dose of 12.5, 25, 50 mg/kg for six hours. Muraglitazar, in a dose-dependent fashion, prevented the development of oedema. In addition, muraglitazar dose-dependently attenuated inflammation and decreased the levels of IL-6, TNFα and iNOS mRNA [1].

Reference:
[1].  Paukkeri, E., Leppnen, T., Lindholm, M., Yam, M., Asmawi, M., & Kolmonen, A. et al. Anti-inflammatory properties of a dual PPARgamma/alpha agonist muraglitazar in in vitro and in vivo models. Arthritis Research & Therapy. 2013;15(2): R51.

Chemical Properties

Cas No. 331741-94-7 SDF
别名 莫格他唑 ,BMS-298585
化学名 N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]-glycine
Canonical SMILES O=C(OC1=CC=C(OC)C=C1)N(CC(O)=O)CC2=CC=C(C=C2)OCCC3=C(C)OC(C4=CC=CC=C4)=N3
分子式 C29H28N2O7 分子量 516.5
溶解度 Chloroform: Slightly Soluble,DMSO: Soluble,Methanol: Slightly Soluble 储存条件 Store at 4°C
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1 mg 5 mg 10 mg
1 mM 1.9361 mL 9.6805 mL 19.3611 mL
5 mM 0.3872 mL 1.9361 mL 3.8722 mL
10 mM 0.1936 mL 0.9681 mL 1.9361 mL
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