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).

• Synonyme(s) : OSC Inhibitor, Ro 48-8071, 4ʹ-(6-(Allylmethylamino)hexyloxy)-4-bromo-2ʹ-fluorobenzophenone, fumarate
• Formule empirique (notation de Hill): C₂₃H₂₇BrFNO₂ · xC₄H₄O₄
• Numéro CAS: 189197-69-1
• Poids moléculaire : 448.37 (free base basis)
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: off-white
• Solubilité: water: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 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
• Clé InChI: CMYCCJYVZIMDFU-UHFFFAOYSA-N

Description

Description générale

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).

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable