Rosiglitazone maleate,155141-29-0

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YZ剂描述：

产品名称：Rosiglitazone maleate

产品别名：马来酸罗格列酮

英文别名：BRL 49653C

靶点：PPARγ

CAS：155141-29-0

纯度：0.99

外观：灰白色固体

保存方法：Store at -20°C

描述：

Rosiglitazone maleate是一种噻唑烷二酮类抗高血糖药，是过氧化物酶体增生物激活受体-γ的高亲和，选择性的激动剂。

溶解性：DMSO : 87 mg/mL (183.9 mM)

体外研究：

Rosiglitazone is an insulin-sensitising agent of the thiazolidinedione class of oral antihyperglycaemic drugs. Rosiglitazone exhibits insulin-sensitising activity 60- to 200-fold higher than that of troglitazone, englitazone, or piogliazone in rodent models of insulin ressitance. Rosiglitazone reduces hyperglycaemia by improving insulin sensitivity in adipose tissue, the liver and skeletal muscle tissue. Such insulin sensitisation may be partly attributable to the effects of Rosiglitazone on the expression of molecules involved in the insulin signalling cascade. In adipose tissue, Rosiglitazone-mediated PPARγ stimulation promotes adipocyte differentiation. Rosiglitazone may also promote the uptake of free fatty acids in adipose tissue, thus reducing systemic free fatty acid levels. The insulin sensitivity of the liver and peripheral tissues may be modulated indirectly by Rosiglitazone-mediated changes in levels of fatty acid or adipocyte-derived factors, such as adiponectin and TNFα. Rosiglitazone may also be involved in modulating the expression of adiponectin receptors in some tissues, which may be relevant to some aspects of insulin sensitisation.

体内研究：

Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats.

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