| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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Purity: ≥98%
Pitavastatin calcium (also called NK-104 Calcium; itavastatin or nisvastatin) is a novel and potent drug of the statin class. Pitavastatin Calcium acts as a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase), resulting 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.
| ln Vitro |
Pitavastatin Calcium either as monolayers (IC50=0.4-5 μM) or spheroids (IC50=0.6-4 μM) suppresses the proliferation of a panel of ovarian cancer cells, including those thought to most likely represent HGSOC[3]. Pitavastatin Calcium (1 μM; 48 hours) promotes apoptosis in Ovcar-8 and Ovcar-3 cells as seen by increased activity of executioner caspases-3, 7, and caspase-8 and caspase-9 [3]. In Ovcar-8 cells, pitavastatin Calcium (1 μM, 48 hours) promotes PARP cleavage [3].
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| ln Vivo |
Regression of the tumor was considerable when pitavastatin Calcium (59 mg/kg; oral; twice daily for 28 days) was administered [3].
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| Cell Assay |
Western Blot Analysis[3]
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)[3]
Doses: 59 mg/kg Route of Administration: po; twice (two times) daily for 28 days Experimental Results: Caused significant tumour regression. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No published information exists on the use of pitavastatin during breastfeeding. It is 99% bound to plasma proteins, so amounts in milk are likely low. Because of a concern with disruption of infant lipid metabolism, the consensus is that pitavastatin should not be used during breastfeeding. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Pitavastatin calcium is the calcium salt of pitavastatin. Used for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise. It has a role as an antioxidant. It is a calcium salt and a statin (synthetic). It contains a pitavastatin(1-).
Pitavastatin Calcium is a calcium salt formulation of pitavastatin, a novel statin that induces plaque regression and elevates HDL-cholesterol levels. See also: Pitavastatin (has active moiety). |
| Molecular Formula |
C50H46CAF2N2O8
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|---|---|---|
| Molecular Weight |
880.98
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| Exact Mass |
880.284
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| CAS # |
147526-32-7
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| Related CAS # |
Pitavastatin;147511-69-1;Pitavastatin-d4;2070009-71-9;Pitavastatin sodium;574705-92-3;Pitavastatin-d4 hemicalcium
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| PubChem CID |
5282451
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| Appearance |
White to off-white solid powder
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| Boiling Point |
692ºC at 760 mmHg
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| Flash Point |
372.3ºC
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| LogP |
6.366
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
63
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| Complexity |
626
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.[Ca+2]
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| InChi Key |
RHGYHLPFVJEAOC-WUVPNHNWSA-L
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| 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+;
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| Chemical Name |
calcium (E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.68 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 (5.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1351 mL | 5.6755 mL | 11.3510 mL | |
| 5 mM | 0.2270 mL | 1.1351 mL | 2.2702 mL | |
| 10 mM | 0.1135 mL | 0.5675 mL | 1.1351 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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