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Pitavastatin Calcium

Catalog No.: GC12116Purity:>99.00%Synonyms: Itabastatin, Itavastatin, NKS 104
ピタバスタチン カルシウム (NK-104 ヘミカルシウム) は、強力なヒドロキシメチルグルタリル CoA (HMG-CoA) レダクターゼ阻害剤です。

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。


Pitavastatin Calcium
Cas No.: 147526-32-7
10mM (in 1mL DMSO)In Stock
$40.00
1
10mgIn Stock
$32.00
1
25mgIn Stock
$50.00
1

引用文献 (Citations)

1 publications本製品を使用した研究者による文献

製品説明 (Description)

Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results 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.

実験プロトコル (Protocol)

Cell experiment [1]:

Cell lines

Huh-7 and SMMC7721 liver cancer cell lines

Preparation method

The solubility of this compound in DMSO is >34.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-20 μM

Applications

In the liver cancer Huh-7 cells and SMMC7721 cells, pitavastatin inhibited cell growth in a dose-dependent way and inhibited colony formation. Pitavastatin significantly arrested the Huh-7 cells at the G1 phase and increased the proportion of sub-G1 phase cells. Pitavastatin induced apoptosis dependent of caspases.

Animal experiment [2]:

Animal models

Experimental autoimmune myocarditis (EAM) BALB/c mice

Dosage form

5 mg/kg; 3 weeks from day 0 to day 21; orally

Application

In experimental autoimmune myocarditis (EAM) BALB/c mice, pitavastatin reduced the pathophysiological severity of the myocarditis. Pitavastatin inhibited the phosphorylation of STAT3 and STAT4, and suppressed production of Th1 cytokine interferon-γ and Th17 cytokine interleukin-17 from autoreactive CD4+T cells in the heart.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] You HY1, Zhang WJ1, Xie XM1, et al. Pitavastatin suppressed liver cancer cells in vitro and in vivo. Onco Targets Ther. 2016 Aug 29;9:5383-8.

[2]. Tajiri K1, Shimojo N, Sakai S, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.

製品資料 (Product Documents)

Purity:>99.00%Appearance:A solid

化学的性質 (Chemical Properties)

CAS番号
147526-32-7
同義語
Itabastatin, Itavastatin, NKS 104
化学名
calcium;(E,3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoate
SMILES
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]
分子式
C50H46CaF2N2O8
分子量
880.98
溶解性
≥ 34.85mg/mL in DMSO
保存条件
4°C, protect from light
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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