499635

OSC Inhibitor, Ro 48-8071

The OSC Inhibitor, Ro 48-8071, also referenced under CAS 189197-69-1, controls the biological activity of 2,3-oxidosqualene:lanosterol cyclase activity (OSC).

• Sinonimo/i: OSC Inhibitor, Ro 48-8071, 4ʹ-(6-(Allylmethylamino)hexyloxy)-4-bromo-2ʹ-fluorobenzophenone, fumarate
• Formula empirica (notazione di Hill): C₂₃H₂₇BrFNO₂ · xC₄H₄O₄
• Numero CAS: 189197-69-1
• Peso molecolare: 448.37 (free base basis)
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: off-white
• Solubilità: water: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C23H27BrFNO2/c1-3-14-26(2)15-6-4-5-7-16-28-20-12-13-21(22(25)17-20)23(27)18-8-10-19(24)11-9-18/h3,8-13,17H,1,4-7,14-16H2,2H3; CMYCCJYVZIMDFU-UHFFFAOYSA-N

Descrizione

Descrizione generale

An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC; IC₅₀ ~ 6.5 nM against mammalian) and reduces cholesterol synthesis (IC₅₀ ~ 1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC₅₀ ~ 10 µM).

An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC; IC₅₀ ~6.5 nM against mammalian) and reduces cholesterol synthesis (IC₅₀ ~1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC₅₀ ~10 µM).

Attenzione

Toxicity: Regulatory Review (Z)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Altre note

Thoma, R., et al. 2004. Nature432, 118.
Peffley, D.M., et al. 1998. Biochem. Pharmacol.56, 439.
Morand, O.H., et al. 1997. J. Lipid Res.38, 373.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable