Rosiglitazone

货号：R2512

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

Peroxisome proliferator activated receptors (PPAR) are nuclear transcriptional factors involved in lipid metabolism with three subtypes: PPARα, PPARγ, and PPARd. Rosiglitazone is a potent PPARγ agonist that binds to the putative ligand binding domain (LBD) of PPARγ with a Kd value of 43 nM. Both isoforms of PPARγ, PPARγ1 and PPARγ2, were activated by rosiglitazone in a dose-dependent manner with EC50 values at 30 nM and 100 nM, respectively. In C3H10T1/2 stem cells treated with 10 μM rosiglitazone for 7 days, the PPARγ expression was up-regulated approximately 3-fold accompanied with significant adipocyte differentiation. In differentiated C3H10T1/2 and 3T3-L1 adipocytes, 1 μM rosiglitazone induced the transcriptions of genes regulating mitochondrial energy metabolism 1 h post dose, and the number of up-regulated genes increased in a time-dependent manner. Uncoupling protein 2 and 3 were stimulated by 1 μM rosiglitazone at 2 h in both adipocytes and remained induced through 28 hours, whereas the transcription of uncoupling protein 1 was not changed. In the examination of mitochondrial heat shock proteins, ribosomal proteins, and translocases of inner and outer mitochondrial membranes, the treatment of 1 μM rosiglitazone for 7 hours induced 23% and 18% of the genes in C3H10T1/2 and 3T3-L1 adipocytes, respectively. In male obese and lean mice treated with 2.5 μmol/kg/d rosiglitazone for one week, the plasma levels of triglycerides, insulin, and glucose of obese mice were reduced to the levels of lean mice. In the analysis of two-dimensional gel electrophoresis of liver samples, rosiglitazone-treated obese mice showed 9 out of 15 upregulated spots characterizing the peroxisome proliferator-like response.

作用机制

Rosiglitazone activates PPARγ via binding to the putative ligand binding domain of PPARγ to alter the expression of downstream genes.

产品信息

CAS号	122320-73-4
分子式	C18H19N3O3S
分子量	357.43
溶解度	DMSO	71.0 mg/mL (198.6 mM)
	Water	lnsoluble
	Ethanol	lnsoluble