| Size | Price | Stock | Qty |
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| 10mg |
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Pitavastatin (NK-104) is a drug of statin class acting as a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor with a variety of biological activity including anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
| ln Vitro |
Pitavastatin suppresses the development of a panel of ovarian cancer cells cultured as spheroids (IC50 = 0.6-4 μM) or as monolayers (IC50 = 0.4-5 μM), including those thought to most likely represent HGSOC[4]. The increased activity of executioner caspases-3,7, as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells, indicates that pitavastatin (one microgram; 48 hours) triggers apoptosis[4]. Ovcar-8 cells cleave PARP when exposed to 1 μM pitavastatin for 48 hours[4]. In TNF-stimulated human saphenous vein endothelial cells, pitavastatin (0.1 and 1 μM; 1 h, followed by 6 h of TNF-α incubation) enhances the production of ICAM-1 mRNA by inhibiting the NF-κB pathway[6].
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| ln Vivo |
Depressant pitavastatin (59 mg/kg; po; twice daily for 28 days) significantly reduces tumor growth[4]. In a rabbit model of diet-induced severe hyperlipidemia, pitavastatin (0.1 mg/kg; po; daily for 12 weeks) slows the development of atherosclerosis and increases NO bioavailability through eNOS up-regulation and O2-depletion[7].
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| Cell Assay |
Western Blot Analysis[4]
Cell Types: Ovcar-8 cells Tested Concentrations: 1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced PARP cleavage. |
| Animal Protocol |
Animal/Disease Models: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours)[4]
Doses: 59 mg/kg Route of Administration: po ; twice (two times) daily for 28 days Experimental Results: Caused significant tumor regression. Animal/Disease Models: Female New Zealand white rabbits (diet induced severe hyperlipidemia)[7] Doses: 0.1 mg/kg Route of Administration: po; daily for 12 weeks Experimental Results: Retarded the progression of atherosclerosis formation and improved NO bioavailability by eNOS up-regulation and decrease of O2-. |
| References |
[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. [6]. Demir B, et al. The Effects of Pitavastatin on Nuclear Factor-Kappa B and ICAM-1 in Human Saphenous Vein Graft Endothelial Culture. Cardiovasc Ther. 2019 May 2;2019:2549432. [7]. Hayashi T, et al. A new HMG-CoA reductase inhibitor, pitavastatin remarkably retards the progression of high cholesterol induced atherosclerosis in rabbits. Atherosclerosis. 2004 Oct;176(2):255-63. [8]. Sahebkar A, et al. A comprehensive review on the lipid and pleiotropic effects of pitavastatin. Prog Lipid Res. 2021 Nov;84:101127. |
| Molecular Formula |
C25H24FNO4
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|---|---|
| Molecular Weight |
421.46
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| CAS # |
147511-69-1
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| Related CAS # |
Pitavastatin Calcium;147526-32-7;Pitavastatin-d4;2070009-71-9;Pitavastatin-d5 sodium;Pitavastatin sodium;574705-92-3
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| SMILES |
O=C(O)C[C@H](O)C[C@H](O)/C=C/C1=C(C2=CC=C(F)C=C2)C3=CC=CC=C3N=C1C4CC4
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~237.27 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3727 mL | 11.8635 mL | 23.7270 mL | |
| 5 mM | 0.4745 mL | 2.3727 mL | 4.7454 mL | |
| 10 mM | 0.2373 mL | 1.1864 mL | 2.3727 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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