265989-46-6
Chemical Structure
2-Hydroxy atorvastatin calcium salt
- CAS No.: 265989-46-6
- Formula:C33H35FN2O6.1/2Ca
- Molecular Weight:594.69
SMILES: FC1=CC=C(C2=C(C3=CC=CC=C3)C(C(NC4=CC=CC=C4O)=O)=C(C(C)C)N2CC[C@@H](O)C[C@@H](O)CC(O)=O)C=C1.[Ca].[1/2]
Biological Activity: 2-Hydroxy atorvastatin calcium salt is an orally active OATP1B1 substrate and inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase). 2-Hydroxy atorvastatin calcium salt enters cells via OATP1B1-mediated cellular uptake and inhibits de novo hepatic cholesterol synthesis. As an active metabolite of Atorvastatin (HY-B0589), 2-Hydroxy atorvastatin calcium salt contributes to the inhibitory activity against plasma HMG-CoA reductase. 2-Hydroxy atorvastatin calcium salt can be biotransformed into an inactive lactone form, which can be hydrolyzed back to its active acid form chemically or enzymatically. 2-Hydroxy atorvastatin (calcium salt) can be used in the research of hypercholesterolemia[1][2][3][4].
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2-Hydroxy atorvastatin calcium salt | 98.01% | 2-Hydroxy atorvastatin calcium salt is an orally active OATP1B1 substrate and inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase). 2-Hydroxy atorvastatin calcium salt enters cells via OATP1B1-mediated cellular uptake and inhibits de novo hepatic cholesterol synthesis. As an active metabolite of Atorvastatin (HY-B0589), 2-Hydroxy atorvastatin calcium salt contributes to the inhibitory activity against plasma HMG-CoA reductase. 2-Hydroxy atorvastatin calcium salt can be biotransformed into an inactive lactone form, which can be hydrolyzed back to its active acid form chemically or enzymatically. 2-Hydroxy atorvastatin (calcium salt) can be used in the research of hypercholesterolemia. | ||||||||||||||||||||
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Ortho-hydroxy atorvastatin-d5 calcium | Ortho-hydroxy atorvastatin-d5 calcium is the deuterium labeled Ortho-hydroxy atorvastatin (HY-144577). Ortho-hydroxy atorvastatin is the metabolic of Atorvastatin (HY-B0589). | |||||||||||||||||||||
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- [1]. Lau YY, et al. effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clinical pharmacology and therapeutics. 2007 Feb;81(2):194-204. [Content Brief]
- [2]. Borek-Dohalský V, et al. Validated HPLC-MS-MS method for simultaneous determination of atorvastatin and 2-hydroxyatorvastatin in human plasma-pharmacokinetic study. Analytical and bioanalytical chemistry. 2006 Sep;386(2):275-85. [Content Brief]
- [3]. Backman JT, et al. Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites. Clinical pharmacology and therapeutics. 2005 Aug;78(2):154-67. [Content Brief]
- [4]. Lennernäs H, et al. Clinical pharmacokinetics of atorvastatin. Clinical pharmacokinetics. 2003;42(13):1141-60. [Content Brief]
