385581-M

11beta-HSD1 Inhibitor, 10j

The 11beta-HSD1 Inhibitor, 10j, also referenced under CAS 1009373-58-3, controls the biological activity of 11beta-HSD1. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): 11beta-HSD1 Inhibitor, 10j
• Empirical Formula (Hill Notation): C₂₆H₃₃BrN₂O₃
• CAS Number: 1009373-58-3
• Molecular Weight: 501.46
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell permeable, spirocyclic urea that acts as a selective inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) (IC₅₀ of 1.6 nM and 5.3 nM) in enzyme and human adipocyte assays, respectively. Consisting of 2 enantiomers, 10j2 (R Isomer) is shown to be ˜ 2-3X more potent than 10j1 (S Isomer), in both aforementioned assays. 11β-HSD1 activity in the presence of 10j2 (10 mg/kg in animals p.o.) results in an ~80% reduction in the concentration of plasma cortisol over vehicle treated controls.

A cell permeable, spirocyclic urea that acts as a selective inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) (IC₅₀ of 1.6 nM and 5.3 nM) in enzyme and human adipocyte assays, respectively. Consisting of 2 enantiomers, 10j2 (R Isomer) is shown to be ˜ 2-3X more potent than 10j1 (S Isomer), in both aforementioned assays. 11β-HSD1 activity in the presence of 10j2 (10mg/kg in animals p.o.) results in an ˜ 80% reduction in the concentration of plasma cortisol over vehicle treated controls.

Warning

Toxicity: Standard Handling (A)

Other Notes

Tice, C.M., et al. 2009. Bioorg. Med. Chem. Lett.20, 881.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable