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Product Description
– Rosiglitazone-d3 is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].
Web ID
– HY-17386S
Shipping
– Room temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C18H16D3N3O3S
References
– [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]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
CAS Number
– 1132641-22-5
Molecular Weight
– 360.45
SMILES
– O=C(N1)C(CC2=CC=C(OCCN(C3=NC=CC=C3)C([2H])([2H])[2H])C=C2)SC1=O
Clinical Information
– No Development Reported
Research Area
– Cancer; Metabolic Disease; Inflammation/Immunology; Neurological Disease
Solubility
– 10 mM in DMSO
Target
– Autophagy;Ferroptosis;Isotope-Labeled Compounds;PPAR;TRP Channel
Pathway
– Apoptosis;Autophagy;Cell Cycle/DNA Damage;Membrane Transporter/Ion Channel;Neuronal Signaling;Others;Vitamin D Related/Nuclear Receptor
Product type
– Isotope-Labeled Compounds
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