Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
体外研究 (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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
444.52
Formula
C25H19D4FNO.1/2Ca2+
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Mukhtar RY, et al. Pitavastatin. Int J Clin Pract. 2005 Feb;59(2):239-52.
[3]. Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003 Fall;21(3):199-215.
[4]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.
Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
体外研究 (In Vitro)
Pitavastatin inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50=0.4-5 μM) or as spheroids (IC50 = 0.6-4 μM)[4]. Pitavastatin (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[4]. Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 cells[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Morikawa S, et al. Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells. J Atheroscler Thromb. 2000;7(3):138-44.
[2]. Katsuki S, et al. Nanoparticle-mediated delivery of pitavastatin inhibits atherosclerotic plaque destabilization/rupture in mice by regulating the recruitment of inflammatory monocytes. Circulation. 2014 Feb 25;129(8):896-906.
[3]. Tajiri K, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.
[4]. Hamano T, et al. Pitavastatin decreases tau levels via the inactivation of Rho/ROCK. Neurobiol Aging. 2012 Oct;33(10):2306-20.
[5]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.
Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
体外研究 (In Vitro)
Pitavastatin Calcium inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50 = 0.4-5 μM) or as spheroids (IC50=0.6-4 μM)[3]. Pitavastatin Calcium (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[3]. Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 cells[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Mukhtar RY, et al. Pitavastatin. Int J Clin Pract. 2005 Feb;59(2):239-52.
[2]. Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003 Fall;21(3):199-215.
[3]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.