Atorvastatin Calcium (CI-981)

N.º de catálogoS2077 Lote:S207705

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Datos técnicos

Fórmula

2(C33H34FN2O5).Ca
Peso molecular 1155.34 Número CAS 134523-03-8
Solubilidad (25°C)* In vitro DMSO 100 mg/mL (86.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Agregue los solventes al producto individualmente y en orden.)
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 significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción Atorvastatin Calcium es un inhibidor de la HMG-CoA reductase utilizado como medicamento para reducir el colesterol que bloquea la producción de colesterol. Atorvastatin Calcium induce apoptosis y autophagy.
Objetivos
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.

Protocolo (de referencia)

Ensayo celular:

[1]
  • Líneas celulares

    BAECs

  • Concentraciones

    10 μM

  • Tiempo de incubación

    24 h

  • Método

    Cells were treated with indicated concentration of the drug for 24 hour.
Estudio en animales:

[5]
  • Modelos animales

    Male New Zealand White rabbits

  • Dosificaciones

    3 mg/kg

  • Administración

    p.o.

Referencias

  • 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/

Validación de productos por parte del cliente

<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>

Datos de [ BMC Pharmacol Toxicol , 2013 , 14, 15 ]

Selleck's Atorvastatin Calcium (CI-981) Ha sido citado por 25 Publicaciones

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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
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Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704

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