Rosiglitazone-d₃

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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].

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Rosiglitazone-d<sub>3</sub> Chemical Structure

Rosiglitazone-d₃ Chemical Structure

CAS No. : 1132641-22-5

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Other Forms of Rosiglitazone-d₃:

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•Related Proteins:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
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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].
In Vitro	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Rosiglitazone-d₃ Related Antibodies
Molecular Weight	360.45
Formula	C₁₈H₁₆D₃N₃O₃S
CAS No.	1132641-22-5
Unlabeled CAS	122320-73-4
SMILES	O=C(N1)C(CC2=CC=C(OCCN(C3=NC=CC=C3)C([2H])([2H])[2H])C=C2)SC1=O
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (270 KB) Handling Instructions (2659 KB)
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief] [2]. 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. [Content Brief] [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. [Content Brief] [4]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [Content Brief] [5]. 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. [Content Brief] [6]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. [Content Brief]