Atorvastatin Calcium (CI-981)

Katalognr.S2077 Batch:S207704

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Tekniska data

Formel

2(C33H34FN2O5).Ca
Molekylvikt 1155.34 CAS-nr. 134523-03-8
Löslighet (25°C)* In vitro DMSO 100 mg/mL (86.55 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Tillsätt lösningsmedel till produkten individuellt och i ordning.)
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.
* <1 mg/ml betyder svårlösligt eller olösligt.
* Vänligen notera att Selleck testar lösligheten för alla förbindelser internt, och den faktiska lösligheten kan skilja sig något från publicerade värden. Detta är normalt och beror på små variationer mellan olika partier.
* Rumstempererad frakt (Stabilitetstester visar att denna produkt kan fraktas utan några kylåtgärder.)

Beredning av stamlösningar

Biologisk aktivitet

Beskrivning Atorvastatin Calcium är en hämmare av HMG-CoA Reductase som används som kolesterolsänkande medicin som blockerar produktionen av kolesterol. Atorvastatin Calcium inducerar apoptos och autophagy.
Mål
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.

Protokoll (från referens)

Cellanalys:

[1]
  • Cellinjer

    BAECs

  • Koncentrationer

    10 μM

  • Inkubationstid

    24 h

  • Metod

    Cells were treated with indicated concentration of the drug for 24 hour.
Djurstudie:

[5]
  • Djurmodeller

    Male New Zealand White rabbits

  • Doseringar

    3 mg/kg

  • Administrering

    p.o.

Referenser

  • https://pubmed.ncbi.nlm.nih.gov/9637705/
  • https://pubmed.ncbi.nlm.nih.gov/17369473/
  • https://pubmed.ncbi.nlm.nih.gov/10559511/
  • https://pubmed.ncbi.nlm.nih.gov/9690910/
  • https://pubmed.ncbi.nlm.nih.gov/12045173/

Kundvalidering av produkt

<p>Micrographs of hematoxylin and eosin-stained liver sections from untreated and atorvastatin-treated TO mouse. Results of representative experiment of liver specimens incubated in vitro at 37癈 with and without 1.0 礛 atorvastatin for 6 hr is shown. A liver specimen at 0 hr is also shown. Liver structure and cytology are preserved in treated and untreated specimens. Inflammation and cholestasis are absent. (Hematoxylin and eosin, 10?and 40?.</p>

Data från [ BMC Pharmacol Toxicol , 2013 , 14, 15 ]

Sellecks Atorvastatin Calcium (CI-981) Har citerats av 25 Publikationer

Ruxolitinib and Polycation Combination Treatment Overcomes Multiple Mechanisms of Resistance of Pancreatic Cancer Cells to Oncolytic Vesicular Stomatitis Virus [ Journal of Virology, July 27, 2017, e00461-17] PubMed: 28566376
Dual pharmacological targeting of coactivator-associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice [ Br J Pharmacol, 2026, 183(15):4399-4415] PubMed: 42055601
The simultaneous targeted Inhibition of ISG15 and HMGCR disrupts cancer stemness through metabolic collapse and induces synthetic lethality in pancreatic ductal adenocarcinoma [ J Exp Clin Cancer Res, 2025, 44(1):317] PubMed: 41366470
The simultaneous targeted Inhibition of ISG15 and HMGCR disrupts cancer stemness through metabolic collapse and induces synthetic lethality in pancreatic ductal adenocarcinoma [ Journal of Experimental & Clinical Cancer Research, 2025, 317] PubMed: 41366470
Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition [ Journal of Experimental & Clinical Cancer Research, 2025, 317] PubMed: 41151153
Cholesterol metabolism regulated by CAMKK2-CREB signaling promotes castration-resistant prostate cancer [ Cell Reports, 2025, 115792] PubMed: 40483692
Cholesterol metabolism regulated by CAMKK2-CREB signaling promotes castration-resistant prostate cancer [ Cell Rep, 2025, 44(6):115792] PubMed: 40483692
The Molecular Chaperone TCP1 Affects Carcinogenicity and Is a Potential Therapeutic Target for Acute Myeloid Leukemia [ Pharmaceutics, 2025, 17(5)557] PubMed: 40430849
Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition [ Neoplasia, 2025, 70:101243] PubMed: 41151153
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704

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