Atorvastatin Calcium.|134523-03-8|(阿托伐他汀钙; CI-981; Atorvastatin hemicalcium)-陌孚医药/Medlife

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Atorvastatin Calcium. (Synonyms: 阿托伐他汀钙; CI-981; Atorvastatin hemicalcium)

目录号: PC12517 纯度: ≥98%

CAS No. :134523-03-8

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PC12517-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称	Atorvastatin Calcium.
中文别名	阿托伐他汀钙;7-[2-(4-氟苯基)-3-苯基-4-(苯胺基甲酰基)-5-(2-丙基)吡咯-1-基]-3,5-二羟基庚酸钙;阿伐他汀钙;[R,(R﹡,R﹡)]-2-(4-氟苯基 )-β,α-二羟基-5-(1-甲基乙基)-3-苯基-[(苯胺基)-羟基]-1H-吡咯-1-庚酸钙盐;Atorvastatin calcium 阿托伐他汀钙;阿伐他汀;阿托伐他丁钙;阿托伐他汀钙阿托伐他汀钙含量阿托伐他汀钙;阿托伐他汀钙标准品;阿托伐他汀钙（无定形的）;阿托伐他汀钙的盐标准品;阿托伐他汀钙及杂质;阿托伐他汀钙盐;阿托伐他汀钙杂质对照品;奥美沙坦甲酮;[R,(R﹡,R﹡)]-2-(4-氟苯基 )-Β,Α-二羟基-5-(1-甲基乙基)-3-苯基-[(苯胺基)-羟基]-1H-吡咯-1-庚酸钙盐(2:1)(结晶型);阿托伐他汀钙,阿伐他汀;氟伐他汀;阿托伐他汀钙,医药级,纯度:>99%
英文名称	Atorvastatin Calcium
英文别名	Atorvastatin Calcium;ATORVASTATIN CA;[r-(r, r)]-7-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-(phenylaminocarbonyl)-1h-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid calcium salt;1h-pyrrole-1-heptanoicacid,beta,delta-dihydroxy-2-(4-fluorophenyl)-5-(1-methy calciumsalt(2:1),(r-(r,r))-lethyl)-3-phenyl-4-((phenylamino)carbonyl);delta-dihydroxy-2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-betcalci1h-pyrrole-1-heptanoicaci;pd134298-38a;ATORVASTATINCALCUIM;calcium (3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-yl-pyrrol-1-yl]-3,5-dihydroxy-heptanoate;1H-Pyrrole-1-heptanoic acid, 2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-calcium salt (2:1), (R-(R,R))-;1H-Pyrrole-1-heptanoic acid;beta,delta-dihydroxy-2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-calcium salt (2:1);(R-(R,R))-, Atorvastatin calcium;Atorvastatin calcium (USAN);Atorvastatin calcium salt;Atorvastatin calcium [USAN];C08078;Calcium (betaR,deltaR)-2-(p-fluorophenyl)-beta,delta-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrole-1-heptanoate (1:2);CI-981;D00887;DRG-0321;Lipibec;Lipitor;Lipitor (TN);LS-136974;Prevencor;Sortis;Tahor;Torvast;YM-548;Atorvastatin Calsium;Atorvastatin calcium salt trihydrate;(3R ,5R )-7-[2-(4-Fluorophenyl)-5-Isopropyl-3-Phenyl-4-(Pheynylcarbamoyl)Pyrrol-1-yl]-3,5-Dihydroheptanoic Acid,calcium salt (2:1) Trihydrate;Atorvastatin (calcium salt);Atorvastatin Calcium( Lipitor®, Stator®, Atoris®, Sortis®);Atorvastatin hemicalcium;Atorvastatin hemicalcium salt;Atorvastatins Calcium;Atorvastatins Calcium amorphous;Calcium (3R,5R)-7-(2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoate;atorvastatin;Cardyl;Tozalip;Xavator;Sotis;Atorvastatin [INN:BAN];Liprimar;Tulip;C33H35FN2O5;(3R,5R)-7-(2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoic acid;A0JWA85V8F;(R-(R,R))-2-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid;Xarator;(betaR,;Atorvastatincalcium
Cas No.	134523-03-8
分子式	C₃₃H₃₅FN₂O₅
分子量	558.64
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

性状

Solid

体外研究(In Vitro)

Atorvastatin treatment decreases apoptosis of myocardial cells by down-regulating GRP78, caspase-12 and CHOP expression in myocardial cells after myocardial infarction, and the endoplasmic reticulum (ER) stress is activated in response to heart failure and angiotensin II (Ang II) stimulation.

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

体内研究(In Vivo)

Atorvastatin (20-30 mg/kg; oral gavage; once a day; for 28 days; ApoE mice) treatment significantly reduces endoplasmic reticulum (ER) stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax in the Ang II-induced ApoE-/- mice. Proinflammatory cytokines such as IL-6, IL-8, IL-1β are all remarkably inhibited after Atorvastatin treatment.

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

Animal Model:	Forty 8-week-old ApoE mice induced with angiotensin II (Ang II)
Dosage:	20 mg/kg, 30 mg/kg
Administration:	Oral gavage; once a day; for 28 days
Result:	Significantly reduced ER stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax in the Ang II-induced ApoE mice. Proinflammatory cytokines such as IL-6, IL-8, IL-1β were all remarkably inhibited

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

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

ClinicalTrial

参考文献

[1]. Santodomingo-Garzón T, et al. Atorvastatin inhibits inflammatory hypernociception. Br J Pharmacol. 2006 Sep;149(1):14-22. [Information]

[2]. Turner NA, et al. Comparison of the efficacies of five different statins on inhibition of human saphenous vein smooth muscle cell proliferation and invasion. J Cardiovasc Pharmacol. 2007 Oct;50(4):458-61. [Information]

[3]. Nawrocki, J.W., et al., Reduction of LDL cholesterol by 25% to 60% in patients with primary hypercholesterolemia by atorvastatin, a new HMG-CoA reductase inhibitor. Arterioscler Thromb Vasc Biol, 1995. 15(5): p. 678-82. [Information]

[4]. Song XJ, et al. Atorvastatin inhibits myocardial cell apoptosis in a rat model with post-myocardial infarction heart failure by downregulating ER stress response. Int J Med Sci. 2011;8(7):564-72. [Information]

[5]. Li Y, et al. Inhibition of endoplasmic reticulum stress signaling pathway: A new mechanism of statins to suppress the development of abdominal aortic aneurysm. PLoS One. 2017 Apr 3;12(4):e0174821. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (86.55 mM)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" 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	1.7311 mL	8.6555 mL	17.3109 mL
5 mM	0.3462 mL	1.7311 mL	3.4622 mL
10 mM	0.1731 mL	0.8655 mL	1.7311 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)。-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 (4.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.33 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% corn oil
Solubility: ≥ 2.5 mg/mL (4.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.33 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。

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Data Sheet

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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