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Rosiglitazone-d4

CAT: 0804-HY-17386S1Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-17386S1Size:1 mg
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Description
Rosiglitazone-d4 is deuterated labeled Rosiglitazone. Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
CAS Number
1132641-21-4
Product Name Alternative
BRL 49653-d4
UNSPSC
12352005
Target
Apoptosis; Autophagy; Ferroptosis; Isotope-Labeled Compounds; PPAR; TRP Channel
Type
Isotope-Labeled Compounds
Related Pathways
Apoptosis; Autophagy; Cell Cycle/DNA Damage; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; Others; Vitamin D Related/Nuclear Receptor
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Cancer; Metabolic Disease; Inflammation/Immunology; Neurological Disease
Solubility
10 mM in DMSO
Smiles
O=C(N1)SC(CC2=CC=C(OC([2H])([2H])C([2H])([2H])N(C)C3=NC=CC=C3)C=C2)C1=O
Molecular Formula
C18H15D4N3O3S
Molecular Weight
361.45
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]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. |[3]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.|[4]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. |[5]Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134 (3) :463-70.|[6]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.|[7]Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96 (3) :215-220.|[8]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported