Synonym
Pitavastatin Calcium; Livalo; NK-104; Pitavastatin hemicalcium; Nisvastatin; NK 104; NK-104; P 872441; P-872441; pitavastatin;
IUPAC/Chemical Name
calcium (E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate
InChi Key
RHGYHLPFVJEAOC-WUVPNHNWSA-L
InChi Code
InChI=1S/2C25H24FNO4.Ca/c2*26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31;/h2*1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31);/q;;+2/p-2/b2*12-11+;
SMILES Code
C1CC1C2=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]
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS#
CAS#147526-32-7 (Pitavastatin Calcium )
CAS#147511-69-1 (Pitavastatin free acid)
CAS#141750-63-2 (Pitavastatin lactone)
Biological target:
Pitavastatin Calcium (NK-104 hemicalcium) is a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor.
In vitro activity:
To investigate how pitavastatin inhibited growth of liver cancer cells, cell cycle distribution of the cells after pitavastatin treatment was measured. Pitavastatin dramatically arrested the Huh-7 cells at the G1 phase (Figure 2A and B). Further analysis found that pitavastatin robustly increased the proportion of sub-G1 phase cells as well as the sub-G1 phase indicated that the cells were going apoptosis (Figure 2C). Pitavastatin may inhibit the growth of liver cancer cells by both arresting the cells at the G0 phase and inducing apoptosis of cells.
Reference: Onco Targets Ther. 2016 Aug 29;9:5383-8. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010166/
In vivo activity:
To investigate whether pitavastatin showed in vivo inhibitory effect, drug-pretreated Huh-7 cells were injected into the rear back subcutaneously. Pitavastatin treatment decreased the growth of liver tumor in nude mice (Figure 4A). It prolonged the survival time of tumor-bearing mice as well (Figure 4B).
Reference: Onco Targets Ther. 2016 Aug 29;9:5383-8. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010166/
|
Solvent |
mg/mL |
mM |
Solubility |
DMSO |
25.0 |
28.40 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
880.98
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. You HY, Zhang WJ, Xie XM, Zheng ZH, Zhu HL, Jiang FZ. Pitavastatin suppressed liver cancer cells in vitro and in vivo. Onco Targets Ther. 2016 Aug 29;9:5383-8. doi: 10.2147/OTT.S106906. PMID: 27621652; PMCID: PMC5010166.
2. Ishihara Y, Ohmori K, Mizukawa M, Hasan AU, Noma T, Kohno M. Beneficial direct adipotropic actions of pitavastatin in vitro and their manifestations in obese mice. Atherosclerosis. 2010 Sep;212(1):131-8. doi: 10.1016/j.atherosclerosis.2010.04.019. Epub 2010 Apr 21. PMID: 20466374.
In vitro protocol:
1. You HY, Zhang WJ, Xie XM, Zheng ZH, Zhu HL, Jiang FZ. Pitavastatin suppressed liver cancer cells in vitro and in vivo. Onco Targets Ther. 2016 Aug 29;9:5383-8. doi: 10.2147/OTT.S106906. PMID: 27621652; PMCID: PMC5010166.
2. Ishihara Y, Ohmori K, Mizukawa M, Hasan AU, Noma T, Kohno M. Beneficial direct adipotropic actions of pitavastatin in vitro and their manifestations in obese mice. Atherosclerosis. 2010 Sep;212(1):131-8. doi: 10.1016/j.atherosclerosis.2010.04.019. Epub 2010 Apr 21. PMID: 20466374.
In vivo protocol:
1. You HY, Zhang WJ, Xie XM, Zheng ZH, Zhu HL, Jiang FZ. Pitavastatin suppressed liver cancer cells in vitro and in vivo. Onco Targets Ther. 2016 Aug 29;9:5383-8. doi: 10.2147/OTT.S106906. PMID: 27621652; PMCID: PMC5010166.
2. Ishihara Y, Ohmori K, Mizukawa M, Hasan AU, Noma T, Kohno M. Beneficial direct adipotropic actions of pitavastatin in vitro and their manifestations in obese mice. Atherosclerosis. 2010 Sep;212(1):131-8. doi: 10.1016/j.atherosclerosis.2010.04.019. Epub 2010 Apr 21. PMID: 20466374.
1: Shang D, Deng S, Yao Z, Wang Z, Ni X, Zhang M, Hu J, Lu H, Zhu X, Huang W, Qiu C, Wen Y. The effect of food on the pharmacokinetic properties and bioequivalence of two formulations of pitavastatin calcium in healthy Chinese male subjects. Xenobiotica. 2016 Jan;46(1):34-9. doi: 10.3109/00498254.2015.1046153. Epub 2015 Jul 17. PubMed PMID: 26186644.
2: Luo Z, Zhang Y, Gu J, Feng P, Wang Y. Pharmacokinetic Properties of Single- and Multiple-Dose Pitavastatin Calcium Tablets in Healthy Chinese Volunteers. Curr Ther Res Clin Exp. 2015 Mar 3;77:52-7. doi: 10.1016/j.curtheres.2015.02.001. eCollection 2015 Dec. PubMed PMID: 26082816; PubMed Central PMCID: PMC4460194.
3: Zhao J, Yan HM, Li Y, Wang J, Han L, Wang ZH, Tang MX, Zhang W, Zhang Y, Zhong M. Pitavastatin calcium improves endothelial function and delays the progress of atherosclerosis in patients with hypercholesterolemia. J Zhejiang Univ Sci B. 2015 May;16(5):380-7. doi: 10.1631/jzus.B1400181. PubMed PMID: 25990055; PubMed Central PMCID: PMC4432990.
4: Yee LL, Wright EA. Pitavastatin calcium: clinical review of a new antihyperlipidemic medication. Clin Ther. 2011 Aug;33(8):1023-42. doi: 10.1016/j.clinthera.2011.07.011. Epub 2011 Aug 4. Review. PubMed PMID: 21816477.
5: Yan HM, Zhao J, Ma DZ, Wang H, Wang J, Wang ZH, Li L, Zhang Y, Zhang W, Zhong M. The effect of pitavastatin calcium on endothelial dysfunction induced by hypercholesterolemia. Expert Opin Pharmacother. 2011 Jul;12(10):1463-71. doi: 10.1517/14656566.2011.583238. PubMed PMID: 21651447.
6: Hussar DA, Christian ME. New drugs: pitavastatin calcium, vigabatrin, and romidepsin. J Am Pharm Assoc (2003). 2010 Jul-Aug;50(4):548-51. doi: 10.1331/JAPhA.2010.10530. PubMed PMID: 20621877.