Pitavastatin calcium

SKU: orb1226205

Description

Pitavastatin calcium is a novel member of the medication class of statins. The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis. Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM). It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions. Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.(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).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.Pitavastatin (1 μM, 48 hours) causes PARP cleavage in Ovcar-8 cells.(In Vivo):Pitavastatin Calcium (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 147526-32-7
• MW: 880.98
• Purity: >98% (HPLC)
• Formula: C₅₀H₄₆CaF₂N₂O₈
• 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]
• Target: cholesterol esters
• Solubility: DMSO: 51 mg/mL (57.89 mM)

Bioactivity

• In Vivo:
  Animal model: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours). Dosage: 59 mg/kg. Administration: p.o. ; twice daily for 28 days. Result: Caused significant tumour regression.
• In Vitro:
  Western blot analysis. Cell line: Ovcar-8 cells. Concentration: 1 μM. Incubation time: 48 hours. Result: Induced PARP cleavage.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Itabastatin | Itavastatin | NK 104

Quick Database Links

Gene Symbol

cholesterol esters