A thazolidinedione agonist of PPARγ; binds to the LBD of PPARγ (Kd = 43 nM); selectively activates chimeras containing the LBDs of PPARγ over PPARα and PPARδ in a cell-based reporter assay at 10 μM; activates full-length PPARγ1 and PPARγ2 in a reporter assay (EC50s = 30 and 100 nM

Rosiglitazone – 25 mg

Brand:
Cayman
CAS:
122320-73-4
Storage:
-20
UN-No:
Non-Hazardous - /

Rosiglitazone is a thiazolidinedione agonist of peroxisome proliferator-activated receptor γ (PPARγ) that binds to the ligand binding domain (LBD) of PPARγ with a Kd value of 43 nM.{8461} It selectively activates chimeras containing the LBDs of PPARγ over PPARα and PPARδ in a cell-based reporter assay when used at a concentration of 10 mM. Rosiglitazone also activates full-length PPARγ1 and PPARγ2 in a reporter assay (EC50s = 30 and 100 nM, respectively). It induces differentiation of C3H10T1/2 stem cells to adipocytes when used at a concentration of 1 μM. Rosiglitazone (4 mg/kg) decreases hemoglobin A1c (HbA1c) and fasting blood glucose levels in a rat model of type 2 diabetes induced by streptozotocin (STZ; Item No. 13104) and a high-carbohydrate/high-fat diet.{16286} It also inhibits increases in contusion volume, macrophage infiltration and activation of microglia, and expression of IL-6, MCP1, ICAM1, caspase-3, and Bax in mouse cerebral cortex in a model of traumatic brain injury induced by controlled cortical impact when administered at a dose of 6 mg/kg.{37783} Formulations containing rosiglitazone have been used to improve glycemic control in the treatment of type 2 diabetes.  

 

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Description

A thazolidinedione agonist of PPARγ; binds to the LBD of PPARγ (Kd = 43 nM); selectively activates chimeras containing the LBDs of PPARγ over PPARα and PPARδ in a cell-based reporter assay at 10 μM; activates full-length PPARγ1 and PPARγ2 in a reporter assay (EC50s = 30 and 100 nM, respectively); induces differentiation of C3H10T1/2 stem cells to adipocytes at 1 μM; decreases HbA1c and fasting blood glucose levels in a rat model of type 2 diabetes induced by STZ and a high-carbohydrate/high-fat diet at 4 mg/kg; inhibits increases in contusion volume, macrophage infiltration and activation of microglia, and expression of IL-6, MCP1, ICAM1, caspase-3, and Bax in mouse cerebral cortex in a model of traumatic brain injury induced by controlled cortical impact at 6 mg/kg

Formal name: 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione

Synonyms:  BRL 49653

Molecular weight: 357.4

CAS: 122320-73-4

Purity: ≥98%

Formulation: A crystalline solid

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