Pitavastatin Lactone-d4

Pitavastatin lactone-d4 is intended for use as an internal standard for the quantification of pitavastatin lactone (Item No. 21785) by GC- or LC-MS. Pitavastatin lactone is a major phase 2 metabolite of the HMG-CoA reductase inhibitor pitavastatin (Item No. 15414).1,2 Pitavastatin lactone is formed when pitavastatin undergoes glucuronidation by the UDP-glucuronysyltransferase (UGT) isoforms UGT1A1, UGT1A3, or UGT2B7 to form pitavastatin glucuronide, which then undergoes non-enzymatic conversion to pitavastatin lactone. It can be retroconverted to pitavastatin via hydrolysis.WARNING This product is not for human or veterinary use.

[1] H FUJINO. Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: human UDP-glucuronosyltransferase enzymes involved in lactonization.[J]. Xenobiotica, 2003, 33 1: 27-41. DOI: 10.1080/0049825021000017957
[2] T AOKI. Pharmacological profile of a novel synthetic inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.[J]. Arzneimittel-Forschung-Drug Research, 1997, 47 8: 904-909.