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Simvastatin acid calcium hydrate

Names

[ CAS No. ]:
530112-57-3

[ Name ]:
Simvastatin acid calcium hydrate

[Synonym ]:
UNII-QSL5L73L0O
Tenivastatin calcium hydrate

Biological Activity

[Description]:

Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR)
Research Areas >> Inflammation/Immunology

[Target]

HMG-CoA reductase, Reactive oxygen species[1][2]


[In Vitro]

Simvastatin acid (0.1-20 μM; 24 h) significantly decreases ROS production between 8.9% and 43% in Indoxyl sulfate-treated hCM cells[2]. Simvastatin acid (0.1-20 μM; 24 h) alters the protein expression of OATP3A1 in hCMs and OATP3A1-expressing HEK293 cells[2]. Western Blot Analysis[2] Cell Line: hCM and HEK293 (transfected with OATP3A1) Concentration: 0.1, 1, 10 and 20 μM Incubation Time: 24 h Result: Decreased 1.5% to 90% in OATP3A1 expression with a dose-dependent manner in both hCMs and OATP3A1-expressing cells.

[References]

[1]. Eduardo Filipe Oliveira, et al. HMG-CoA Reductase inhibitors: an updated review of patents of novel compounds and formulations (2011-2015). Expert Opin Ther Pat. 2016 Nov;26(11):1257-1272.

[2]. Atilano-Roque A, et al. Characterization of simvastatin acid uptake by organic anion transporting polypeptide 3A1 (OATP3A1) and influence of drug-drug interaction. Toxicol In Vitro. 2017 Dec;45(Pt 1):158-165.

Chemical & Physical Properties

[ Molecular Formula ]:
C50H84CaO15

[ Molecular Weight ]:
965.27100

[ Exact Mass ]:
964.54400

[ PSA ]:
241.47000

[ LogP ]:
5.34910


Related Compounds