Rosiglitazone

Biological Activity

Rosiglitazone, also known as BRL 49653, is a potent and selective agonist for PPARγ (Peroxisome proliferator-activated receptor) with an EC50 of 43 nM. PPARγ plays a functional role in adipogenesis, it belongs to a group of nuclear receptor proteins that are essential to the regulation of cellular differentiation, development and metabolism. Rosiglitazone binds to the PPAR receptors in fat cells and making the cells more responsive to insulin. It activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC50 values of approximately 30 nM and 100 nM, respectively. Rosiglitazone induced adipocyte differentiation in pluripotent C3H10T1/2 stem cells. Rosiglitazone suppressed the activity of complex I of the MRC in ob/ob mice, but did not affect beta-oxidation.

Product Citations

• 

  Adv Sci (Weinh). 2023 Mar 27;e2207224.

  Hypoxia Drives Material‐Induced Heterotopic Bone Formation by Enhancing Osteoclastogenesis via M2/Lipid‐Loaded Macrophage Axis
  Rosiglitazone purchased from AbMole

• 

  Biomaterials. 2023 Oct 17.

  The genetic background determines material-induced bone formation through the macrophage-osteoclast axis
  Rosiglitazone purchased from AbMole

• 

  Food Res Int. 2023 Jan 17;112486.

  Evaluation the food safety of cultured fat via detection of residues of adipogenic differentiation cocktail in cultured fat with high performance liquid chromatography and enzyme-linked immunosorbent assay
  Rosiglitazone purchased from AbMole

• 

  Food Res Int. 2023 Feb 14.

  N-acetylcysteine promotes the proliferation of porcine adipose-derived stem cells during in vitro long-term expansion for cultured meat production
  Rosiglitazone purchased from AbMole

• 

  J Agric Food Chem. 2023 Feb 24.

  Preparation and Quality Evaluation of Cultured Fat
  Rosiglitazone purchased from AbMole

• 

  Food Res Int. 2022 Oct;160:111636.

  Production of cultured fat with peanut wire-drawing protein scaffold and quality evaluation based on texture and volatile compounds analysis
  Rosiglitazone purchased from AbMole

• 

  Food Res Int. 2022 Sep 14.

  Identification of porcine adipose progenitor cells by fluorescence-activated cell sorting for the preparation of cultured fat by 3D bioprinting
  Rosiglitazone purchased from AbMole

• 

  Biosci Biotechnol Biochem. 2022 Feb 24;86(3):331-339.

  BRCC36 promotes intestinal mucosal barrier injury caused by BMP2 after ischemia reperfusion via inhibiting PPARγ signaling
  Rosiglitazone purchased from AbMole

Chemical Information

Molecular Weight	357.43
Formula	C18H19N3O3S
CAS Number	122320-73-4
Solubility (25°C)	DMSO 20 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] García-Ruiz I, et al. Hepatology. Effects of rosiglitazone on the liver histology and mitochondrial function in ob/ob mice.