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).

• Synonym(s): OSC Inhibitor, Ro 48-8071, 4ʹ-(6-(Allylmethylamino)hexyloxy)-4-bromo-2ʹ-fluorobenzophenone, fumarate
• Empirical Formula (Hill Notation): C₂₃H₂₇BrFNO₂ · xC₄H₄O₄
• CAS Number: 189197-69-1
• Molecular Weight: 448.37 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: off-white
• solubility: water: 5 mg/mL
• shipped in: ambient
• storage temp.: 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
• InChI key: CMYCCJYVZIMDFU-UHFFFAOYSA-N

Description

General description

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).

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable