1132641-21-4
1132641-21-4
Chemical Structure
Rosiglitazone-d4
Synonym(s): BRL 49653-d4
- CAS No.: 1132641-21-4
- Formula:C18H15D4N3O3S
- Molecular Weight:361.45
InChIKey: YASAKCUCGLMORW-MKQHWYKPSA-N
SMILES: O=C(N1)SC(CC2=CC=C(OC([2H])([2H])C([2H])([2H])N(C)C3=NC=CC=C3)C=C2)C1=O
Biological Activity: Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). 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].
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Rosiglitazone-d4 | Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). 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. | |||||||||||||||||||||
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Rosiglitazone (Standard) | 99.59% | Rosiglitazone (Standard) is the analytical standard of Rosiglitazone. This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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Rosiglitazone-d4-1 | Rosiglitazone-d4-1 (BRL 49653-d4-1) is deuterium-labeled Rosiglitazone (HY-17386). | |||||||||||||||||||||
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Rosiglitazone-d3 | 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. | |||||||||||||||||||||
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Rosiglitazone | 99.94% | Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. 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. | ||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;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]
- [4]. 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]
- [7]. 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]
