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385581-M

Sigma-Aldrich

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

Empirical Formula (Hill Notation):
C26H33BrN2O3
CAS Number:
1009373-58-3
Molecular Weight:
501.46
UNSPSC Code:
12352111
NACRES:
NA.77

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

385581-10MG:
385581-MG:
385581-10MG-M:
385581-500MG-M:

Certificates of Analysis (COA)

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