Rosiglitazone maleate is an insulin sensitizer. Rosiglitazone maleate activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC50 values of approximately 30 nM and 100 nM, respectively. Rosiglitazone maleate (Avandia) improves glycemic control while reducing circulating insulin levels. Rosiglitazone maleate also appears to have an anti-inflammatory effect in addition to its effect on insulin resistance. Rosiglitazone maleate is active in vivo as an antidiabetic agent in the ob/ob mouse model, and has been used as an oral hypoglycemic agent in the treatment of Type II diabetes in humans for many years.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
Adherence to a fixed-dose combination of rosiglitazone maleate/metformin hydrochloride in subjects with type 2 diabetes mellitus: a retrospective database analysis.
Vanderpoel DR, et al. Clin Ther. 2004 Dec;26(12):2066-75. PMID: 15823770.
Effects of rosiglitazone maleate when added to a sulfonylurea regimen in patients with type 2 diabetes mellitus and mild to moderate renal impairment: a post hoc analysis.
Agrawal A, et al. Clin Ther. 2003 Nov;25(11):2754-64. PMID: 14693302.
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