Lapaquistat-d9 acetate

Modify Date: 2024-01-19 17:38:09

Lapaquistat-d9 acetate Structure
Lapaquistat-d9 acetate structure
Common Name Lapaquistat-d9 acetate
CAS Number 1292841-28-1 Molecular Weight 654.20
Density N/A Boiling Point N/A
Molecular Formula C33H32D9ClN2O9 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Lapaquistat-d9 acetate


Lapaquistat-d9 acetate (TAK-475-d9) is the deuterium labeled Lapaquistat acetate. Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway[1]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research[2].

 Names

Name Lapaquistat-d9 acetate

 Lapaquistat-d9 acetate Biological Activity

Description Lapaquistat-d9 acetate (TAK-475-d9) is the deuterium labeled Lapaquistat acetate. Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway[1]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research[2].
Related Catalog
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].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Stein EA, et al. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85.

[3]. Marcuzzi A, et al. Repositioning of Tak-475 In Mevalonate Kinase Disease: Translating Theory Into Practice. Curr Med Chem. 2018;25(24):2783-2796.

[4]. M Shiomi, et al. Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions. Br J Pharmacol. 2008 Jul;154(5):949-57.

 Chemical & Physical Properties

Molecular Formula C33H32D9ClN2O9
Molecular Weight 654.20