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Rosiglitazone maleate

Cat. No. M2038

Rosiglitazone maleate Structure

Synonym: Avandia

Size Price Availability Quantity
50mg USD 50 In stock
100mg USD 75 In stock
200mg USD 110 In stock
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Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 473.5
Formula C18H19N3O3S.C4H4O4
CAS Number 155141-29-0
Purity 100.00%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

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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Keywords: Rosiglitazone maleate, Avandia supplier, PPAR, inhibitors

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