331741-94-7 Usage
Description
Muraglitazar is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ (EC50s = 0.32 and 0.11 μM, respectively). It is selective for PPARα/γ over other nuclear receptors, including PPARδ, RXRα, RARs, estrogen receptor α (ERα), ERβ, androgen receptor (AR), and progesterone receptor (PR). Muraglitazar (50 μM) reduces the size of lipid droplets in oleic acid-treated HepaRG human hepatocytes. It reduces plasma levels of glucose, triglycerides, free fatty acids, and insulin by 54, 33, 62, and 48%, respectively, in db/db mice when administered at a dose of 10 mg/kg per day. Muraglitazar (10 mg/kg per day) reduces plasma levels of glucose, triglycerides, and cholesterol in diet-induced obese mice. Muraglitazar also inhibits LPS-induced increases in nitric oxide (NO) production and IL-6, TNF-α, and inducible nitric oxide synthase (iNOS) protein levels in J774 murine macrophages in a concentration-dependent manner. It inhibits carrageenan-induced paw edema in mice when administered at doses ranging from 12.5 to 50 mg/kg.
Chemical Properties
Off-White Solid
Uses
Different sources of media describe the Uses of 331741-94-7 differently. You can refer to the following data:
1. It is a peroxisome proliferator-activated receptor (PPAR) a/ dual agonist
2. It is a peroxisome proliferator-activated receptor (PPAR) α/γ dual agonist.
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].
IC 50
0.42 μm: shows agonistic activity at peroxisome proliferator-activated receptor α (pparα)
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 331741-94-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,1,7,4 and 1 respectively; the second part has 2 digits, 9 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 331741-94:
(8*3)+(7*3)+(6*1)+(5*7)+(4*4)+(3*1)+(2*9)+(1*4)=127
127 % 10 = 7
So 331741-94-7 is a valid CAS Registry Number.
InChI:InChI=1/C29H28N2O7/c1-20-26(30-28(37-20)22-6-4-3-5-7-22)16-17-36-24-10-8-21(9-11-24)18-31(19-27(32)33)29(34)38-25-14-12-23(35-2)13-15-25/h3-15H,16-19H2,1-2H3,(H,32,33)
331741-94-7Relevant articles and documents
Identification of by-products in support of process development of Muraglitazar
Pathirana, Charles,Rusowicz, Andrew,Suda, Russell,Swaminathan, Shankar,Palaniswamy, Venkatapuram
, p. 283 - 288 (2017/03/16)
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PROCESS OF PREPARING SUBSTITUTED CARBAMATES AND INTERMEDIATES THEREOF
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Page/Page column 16-18, (2008/06/13)
An improved process of preparing substituted carbamate derivatives, and crystalline forms thereof, useful for the treatment of dyslipidemia and diabetes, and intermediates thereof are provided.
