Rosiglitazone (maleate)
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5) .
Product Specifications
CAS Number
[155141-29-0]
Product Name Alternative
BRL 49653C
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
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
COVID-19-anti-virus
Field of Research
Cancer; Metabolic Disease; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/rosiglitazone-maleate.html
Purity
99.73
Solubility
DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic)
Smiles
O=C(O)/C=C\C(O)=O.CN(CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)C3=CC=CC=N3
Molecular Formula
C22H23N3O7S
Molecular Weight
473.50
Precautions
H302, H315, H319, H335
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PPARγ
Citation 01
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