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Atorvastatin Calcium

Name: Atorvastatin Calcium
Brand: Selleck Chemicals
SKU: S2077
Rating: 5 (10 reviews)

Catalog No.S2077 Purity:99.98%

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.

Atorvastatin Calcium Chemical Structure

CAS No. 134523-03-8

Purity & Quality Control

Batch: Purity: 99.98%

99.98

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Signaling Pathway

HMG-CoA Reductase Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
CHO	Function assay			Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, Ki=0.45μM.	23571415
CHO	Function assay			pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=0.81283μM.	23571415
Me300	Cytotoxicity assay		72 hrs	Cytotoxicity against human Me300 cells after 72 hrs by MTT assay, IC50=1.2μM.	22533316
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=1.97μM.	22533316
CHO	Function assay			Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, Ki=2.58μM.	23571415
CHO	Function assay			pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=3.38844μM.	23571415
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=4.22μM.	22533316
LN18	Cytotoxicity assay		72 hrs	Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=6.9μM.	22533316
LNZ308	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNZ308 cells after 72 hrs by MTT assay, IC50=7.44μM.	22533316
LN229	Cytotoxicity assay		72 hrs	Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=8.1μM.	22533316
Caco2	Cytotoxicity assay		72 hrs	Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay, IC50=18.7μM.	22533316
HCEC	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=20.3μM.	22533316
LN18	Function assay	1 to 3 uM	24 hrs	Inhibition of DNA synthesis in human LN18 cells assessed as inhibition of tritiated thymidine incorporation at 1 to 3 uM after 24 hrs by beta counting	22533316
LN229	Function assay	1 to 3 uM	24 hrs	Inhibition of DNA synthesis in human LN229 cells assessed as inhibition of tritiated thymidine incorporation at 1 to 3 uM after 24 hrs by beta counting	22533316
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

HMG-CoA reductase ^[1]
(Cell-free assay)

In vitro
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]
Cell Research	Cell lines	BAECs
	Concentrations	10 μM
	Incubation Time	24 h
	Method	Cells were treated with indicated concentration of the drug for 24 hour.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Growth inhibition assay	Cell viability		25874930

In Vivo
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]
Animal Research	Animal Models	Male New Zealand White rabbits
	Dosages	3 mg/kg
	Administration	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01555632	Withdrawn	Recurrent Prostate Cancer\|Stage I Prostate Cancer\|Stage IIA Prostate Cancer\|Stage IIB Prostate Cancer\|Stage III Prostate Cancer\|Stage IV Prostate Cancer	University of Nebraska\|National Cancer Institute (NCI)	March 2012	Not Applicable

References

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Chemical Information & Solubility

Molecular Weight	1155.34	Formula	2(C₃₃H₃₄FN₂O₅).Ca
CAS No.	134523-03-8	SDF	Download Atorvastatin Calcium SDF
Smiles	CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4.CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4.[Ca+2]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (86.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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