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
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About This Item
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Quality Level
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
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
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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