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Merck
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Key Documents

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.

别名:

11beta-HSD1 Inhibitor, 10j

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About This Item

经验公式(希尔记法):
C26H33BrN2O3
分子量:
501.46
分類程式碼代碼:
12352111
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze

顏色

white

溶解度

DMSO: 100 mg/mL

儲存溫度

2-8°C

一般說明

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.

警告

Toxicity: Standard Handling (A)

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 2

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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