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Pitavastatin Calcium
酶HMGCR抑制剂,Pitavastatin Calcium是有效的羟甲基戊二酰-CoA (HMG-CoA) 还原酶抑制剂。Pitavastatin Calcium在HepG2细胞中抑制乙酸合成胆固醇的 IC50 为5.8 nM。
目录号: PC12533 纯度: ≥98%
CAS No. :147526-32-7
商品编号 规格 价格 会员价 是否有货 数量
PC12533-10mg 10mg ¥441.00 请登录
PC12533-25mg 25mg ¥705.60 请登录
PC12533-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥539.00 请登录
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中文名称
Pitavastatin Calcium
中文别名
匹伐他汀钙;伊伐他汀;(+)-双{(3R,5S,6E)-7-[2-环丙基-4-(4-氟代苯基)喹啉-3-基]-3,5-二羟基-6-庚烯酸}钙盐 (2:1);匹伐他汀钙 GMP;5-(1H-吲哚基)2-甲基噁唑;阿伐他汀钙;匹伐他汀;匹伐他汀-D4钙盐;匹伐他汀钙盐;双{(3R,5S,6E)-7-[2-环丙基-4-(氟代苯基)喹啉-3-苯基]-3,5-二羟基-6-庚烯酸乙酯}钙盐(2:1);匹法他汀钙;匹伐他汀钙API;匹伐他汀钙无定形;匹伐他汀钙晶型Ⅰ;匹伐他汀钙(标准品);+双{(3R,5S,6E)-7-[2-环丙基-4-(氟代苯基)喹啉-3-苯基]-3,5-二羟基-6-庚烯酸乙酯}钙盐(2:1)
英文名称
Pitavastatin Calcium
英文别名
Pitavastatin calcium;ITAVASTATIN CA;ITAVASTATIN CALCIUM;:(+)-monocalciumbis{(3r,5s,6e)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoate};6-heptenoicacid,7-(2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl)-3,5-dihydro;calciumsalt(2:1),(3r,5s,6e)-xy;nk104;nk104(acid);monocalciumbis[(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-Fluorophenyl)-3-Quinolyl)-3,5-Dihydroxy-6-heptenoate](+)α- Phenethylamine Salt;D01862;PITAVASTATINCALCIUM(FORR&DONLY);(+)-Monocalciumbis{(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoate};PITAVASTATINHEMICALCIUM;Calcium (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl)-3,5-dihydroxyhept-6-enoate;Calcium (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate;Pitavastatin (calcium salt);Pitavastatin CalciumDISCONTINUED;Pitavstatin Calcium;(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid;(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-hept-6-enoic acid;[14C]-Pitavastatin;[3H]-Pitavastatin;Alipza;CHEBI:71258;Livalo;Livazo;Nisvastatin;NK-104;UNII-IYD54XEG3W;[ "" ];NK-104 Calcium;Pitavasttin Calcium;Pitavastatin Calciu;Pitavastatin Calcuim;(+)-Monocalcium bis{(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoate};Pitavastatin;Itavastatin;NK 104;Pitavastatin [INN];C25H24FNO4;M5681Q5F9P;Zypitamag;Flovas;(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid;P 872441;( )-(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy-6-heptenoic acid;NK 104 (acid);Pitavastatin calcium (JAN
Cas No.
147526-32-7
分子式
C25H24FNO4
分子量
421.46
包装储存

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

性状

Solid

IC50 & Target[1][2]

HMG-CoA Reductase

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: Ovcar-8 cells
Concentration: 1?μM
Incubation Time: 48 hours
Result: Induced PARP cleavage.
体内研究(In Vivo)

Pitavastatin Calcium (59?mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 50 mg/mL (113.51 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2702 mL 11.3510 mL 22.7020 mL
5 mM 0.4540 mL 2.2702 mL 4.5404 mL
10 mM 0.2270 mL 1.1351 mL 2.2702 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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