Pitavastatin calcium Inhibitor CAS No. 147526-32-7

Product Name	Pitavastatin calcium
Synonyms	NK-104, itavastatin, nisvastatin
CAS No.	147526-32-7
Molecular Weight	880.98
Formula	C₅₀H₄₆CaF₂N₂O₈
Chemical Structure

Biological activities

Pitavastatin calcium is a calcium salt of pitavastatin which is a synthetic HMG-CoA reductase inhibitor. The IC50 of pitavastatin is 6.8 nM against HMG-CoA reductase.^[1] Pitavastatin produces marked reductions in triglyceride-rich particles (very-low-density [VLDL] and intermediate-density lipoproteins [IDL]).^[2] Pitavastatin diminishes the area of atherosclerotic lesions.^[3] Pitavastatin attenuates the migration activity of smooth muscle cells. Pitavastatin attenuates the PDGF-BB -induced surface expression of LR11 and uPAR. Pitavastatin upregulates the expression of LR11 and SMemb. ^[4] In both basal and ABCA1 expressing cells, pitavastatin 0.1閳?0 µM dose-dependently increases in cholesterol efflux to apoA-I.^[5] Pitavastatin inhibits basal and cytokine-treated EL expression in endothelial cells. Pitavastatin decreases phospholipase activities of endothelial cells, and concomitant treatment with mevalonate reversed its inhibitory effect. Pitavastatin decreases RhoA activity and EL expression in mouse tissues.^[6]

Protocols

In vitro: Pitavastatin is dissolved in DMSO.^[5]

References

[1] Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003, 21(3): 199-215. 閵嗏偓閵嗏偓 [2] Isley, W.L. et al. Pitavastatin (NK-104), a new HMG-CoA reductase inhibitor. Drugs Today, 2001, 37(9): 587. [3] Kitahara M, et al. Atherosclerosis induced by chronic inhibition of the synthesis of nitric oxide in moderately hypercholesterolaemic rabbits is suppressed by pitavastatin. Br J Pharmacol. 2010, 159(7): 1418-1428. 閵嗏偓閵嗏偓 [4] Jiang M, et al. Pitavastatin attenuates the PDGF-induced LR11/uPA receptor-mediated migration of smooth muscle cells. Biochem Biophys Res Commun. 2006, 348(4): 1367-1377. 閵嗏偓閵嗏偓 [5] Kojima Y, et al. Pitavastatin decreases the expression of endothelial lipase both in vitro and in vivo. Cardiovasc Res. 2010, 87(2): 385-393. [6] Kojima Y, et al. Pitavastatin decreases the expression of endothelial lipase both in vitro and in vivo. Cardiovasc Res. 2010, 87(2): 385-393. 閵嗏偓閵嗏偓

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