Name: Atorvastatin Calcium (CI-981)
Brand: Selleck Chemicals
SKU: S2077
Rating: 5 (16 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.98%

99.98

Relaterade mål	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Övrigt HMG-CoA Reductase Inhibitorer	Mevastatin SR-12813 Clinofibrate Dihydrolanosterol 7-ketocholesterol Cerivastatin sodium

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning	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
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Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	1155.34	Formel	2(C₃₃H₃₄FN₂O₅).Ca	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	134523-03-8	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	N/A			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]

Löslighet (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (86.55 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 35%PEG300 2 2%Tween80 3 61%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	4.000mg/ml (3.46mM)	Taking the 1 mL working solution as an example, add 20 μL of 200 mg/ml clarified DMSO stock solution to 350 μL PEG300, mix evenly to clarify it; add 20 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	HMG-CoA reductase (Cell-free assay)
In vitro	Atorvastatin Calcium 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). This compound significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. It downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. The chemical inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. This compound (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. It (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation.
In vivo	Atorvastatin Calcium reduces vascular mRNA expression of p22phox and nox1 and increased aortic catalase expression in statin-treated rats. This compound inhibits the increase of hsCRP serum levels in the cholesterol-fed rabbits. It inhibits the increase in osteopontin expression throughout the valve leaflet in the hypercholesterolemic aortic valves.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/9637705/ [2] https://pubmed.ncbi.nlm.nih.gov/17369473/ [3] https://pubmed.ncbi.nlm.nih.gov/10559511/ [4] https://pubmed.ncbi.nlm.nih.gov/9690910/ [5] https://pubmed.ncbi.nlm.nih.gov/12045173/

Applikationer (Applications)

Metoder	Biomarkörer	Bilder	PMID
Growth inhibition assay	Cell viability		25874930

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Atorvastatin Calcium (CI-981) HMG-CoA Reductase Hämmare

Molekylvikt: 1155.34

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Atorvastatin Calcium (CI-981) HMG-CoA Reductase Hämmare

Molekylvikt: 1155.34

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)