Rosiglitazone (potassium)

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM) . Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].

Product Specifications

CAS Number

[316371-84-3]

Product Name Alternative

BRL 49653 (potassium)

UNSPSC

12352005

Target

Apoptosis; Autophagy; Ferroptosis; PPAR; TRP Channel

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/rosiglitazone-potassium.html

Solubility

10 mM in DMSO

Smiles

CN(C1=NC=CC=C1)CCOC2=CC=C(C=C2)CC3SC([N-]C3=O)=O.[K+]

Molecular Formula

C18H18KN3O3S

Molecular Weight

395.52

References & Citations

[1]Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma) . J Biol Chem. 1995 Jun 2;270 (22) :12953-6. |[2]Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39 (3) :665-8. |[3]Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134 (3) :463-70. |[4]Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79 (6) :1023-30. |[5]Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96 (3) :215-220. |[6]Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. |[7]Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85 (2) :273-284.