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.

• Sinonimo/i: 11beta-HSD1 Inhibitor, 10j
• Formula empirica (notazione di Hill): C₂₆H₃₃BrN₂O₃
• Numero CAS: 1009373-58-3
• Peso molecolare: 501.46
• Codice UNSPSC: 12352111
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Attenzione

Toxicity: Standard Handling (A)

Altre note

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

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 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable