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Pitavastatin Calcium

Catalog No.
A8504
Enzyme HMGCR inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$61.00
In stock
10mg
$55.00
In stock
25mg
$88.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis. Alternate studies show that pitavastatin can suppress oxygen production in endothelial cells by inhibiting NADPH oxidase. In addition, pitavastatin reduces the expression of eNOS mRNA while increasing the NO dependent response stimulated by acetylcholine and the calcium ionophore, A23187. Furthermore, pitavastatin inhibits the up-regulation of conductance calcium-activated potassium channels by lowering cholesterol levels in cells.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt880.98
Cas No.147526-32-7
FormulaC50H46CaF2N2O8
Solubility≥34.85 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Namecalcium;(E,3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoate
SDFDownload SDF
Canonical SMILESC1CC1C2=NC3=CC=CC=C3C(=C2C=CC(CC(CC(=O)[O-])O)O)C4=CC=C(C=C4)F.C1CC1C2=NC3=CC=CC=C3C(=C2C=CC(CC(CC(=O)[O-])O)O)C4=CC=C(C=C4)F.[Ca+2]
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Huh-7 and SMMC7721 liver cancer cell lines

Preparation method

The solubility of this compound in DMSO is >34.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-20 μM

Applications

In the liver cancer Huh-7 cells and SMMC7721 cells, pitavastatin inhibited cell growth in a dose-dependent way and inhibited colony formation. Pitavastatin significantly arrested the Huh-7 cells at the G1 phase and increased the proportion of sub-G1 phase cells. Pitavastatin induced apoptosis dependent of caspases.
Animal experiment [2]:

Animal models

Experimental autoimmune myocarditis (EAM) BALB/c mice

Dosage form

5 mg/kg; 3 weeks from day 0 to day 21; orally

Application

In experimental autoimmune myocarditis (EAM) BALB/c mice, pitavastatin reduced the pathophysiological severity of the myocarditis. Pitavastatin inhibited the phosphorylation of STAT3 and STAT4, and suppressed production of Th1 cytokine interferon-γ and Th17 cytokine interleukin-17 from autoreactive CD4+T cells in the heart.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] You HY1, Zhang WJ1, Xie XM1, et al. Pitavastatin suppressed liver cancer cells in vitro and in vivo. Onco Targets Ther. 2016 Aug 29;9:5383-8.

[2]. Tajiri K1, Shimojo N, Sakai S, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.

Quality Control

Chemical structure

Pitavastatin Calcium

Related Biological Data

Pitavastatin Calcium