Atorvastatin Calcium

製品コードS2077 バッチS207750

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	2(C₃₃H₃₄FN₂O₅).Ca
	分子量	1155.34	CAS No.	134523-03-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (86.55 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
in vitro	Atorvastatin inhibits pre-proET-1 mRNA expression in a concentration- and time-dependent fashion (60-70% maximum inhibition) and reduces immunoreactive ET-1 levels (25-50%), this inhibitory effect is maintained in the presence of oxidized LDL (1-50 mg/mL). ^[1] Atorvastatin significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. Atorvastatin downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. Atorvastatin inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. ^[2] Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. Atorvastatin (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. Atorvastatin (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. ^[3] Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation. ^[4]
in vivo	Atorvastatin reduces vascular mRNA expression of p22phox and nox1 and increased aortic catalase expression in statin-treated rats. ^[2] Atorvastatin inhibits the increase of hsCRP serum levels in the cholesterol-fed rabbits. Atorvastatin inhibits the increase in osteopontin expression throughout the valve leaflet in the hypercholesterolemic aortic valves. ^[5]

製品説明

Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.

in vitro

Atorvastatin inhibits pre-proET-1 mRNA expression in a concentration- and time-dependent fashion (60-70% maximum inhibition) and reduces immunoreactive ET-1 levels (25-50%), this inhibitory effect is maintained in the presence of oxidized LDL (1-50 mg/mL). ^[1]

Atorvastatin significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. Atorvastatin downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. Atorvastatin inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. ^[2]

Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. Atorvastatin (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. Atorvastatin (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. ^[3]

Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation. ^[4]

in vivo

Atorvastatin reduces vascular mRNA expression of p22phox and nox1 and increased aortic catalase expression in statin-treated rats. ^[2]

Atorvastatin inhibits the increase of hsCRP serum levels in the cholesterol-fed rabbits. Atorvastatin inhibits the increase in osteopontin expression throughout the valve leaflet in the hypercholesterolemic aortic valves. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BAECs
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of the drug for 24 hour.
動物実験	動物モデル	Male New Zealand White rabbits
	投薬量	3 mg/kg
	投与方法	p.o.

参考

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カスタマーフィードバック

: Data from [BMC Pharmacol Toxicol, 2013, 14, 15]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Upregulation of the Mevalonate Pathway through EWSR1-FLI1/EGR2 Regulatory Axis Confers Ewing Cells Exquisite Sensitivity to Statins [ Cancers (Basel), 2022, 14(9)2327]	PubMed: 35565457
Ultra-fast proteomics with Scanning SWATH [ Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4]	PubMed: 33767396
The thrombin receptor links brain derived neurotrophic factor to neuron cholesterol production, resiliency and repair after spinal cord injury [ Neurobiol Dis, 2021, 152:105294]	PubMed: 33549720
Atorvastatin potentiates the chemosensitivity of human liver cancer cells to cisplatin via downregulating YAP1 [ Oncol Lett, 2021, 21(2):82]	PubMed: 33363619
The MEK5-ERK5 kinase axis controls lipid metabolism in small cell lung cancer. [ Cancer Res, 2020, canres.1027.2019]	PubMed: 31969375
Exosomes derived from atorvastatin-pretreated MSC accelerate diabetic wound repair by enhancing angiogenesis via AKT/eNOS pathway [ Stem Cell Res Ther, 2020, 11(1):350]	PubMed: 32787917
A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition. [ Nat Commun, 2019, 10(1):96]	PubMed: 30626880
Ruxolitinib and Polycation Combination Treatment Overcomes Multiple Mechanisms of Resistance of Pancreatic Cancer Cells to Oncolytic Vesicular Stomatitis Virus [ J Virol, 2017, 91(16)e00461-17]	PubMed: 28566376
Lovastatin induces apoptosis of HepG-2 cells by activating ROS-dependent mitochondrial and ER stress pathways [ Int J Clin Exp Pathol, 2017, 10(12):11480-11488]	PubMed: 31966503
Bioenergetic study of murine hepatic tissue treated in vitro with atorvastatin. [Alfazari AS, et al. BMC Pharmacol Toxicol, 2013, 14:15]	PubMed: 23448291

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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