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INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rat, and human 11β-HSD1, respectively.


ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

AZD 4017

AZD4017 (AZD-4017) is a potent, selective, and orally bioavailable human 11β-HSD1 with IC50 of 7 nM, shows no significant activity against 11β-HSD1 and 17β-HSD1, 17β-HSD3 (IC50>30 uM).


BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2.

BI 135585

BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.


UE2343 (UE-2343, Xanamem) is a potent, orally bioavailable, brain penetrant 11β-HSD1 inhibitor with IC50 of 24 nM in cell-free assays, with no activity for isozyme 11β-HSD2.


A specific and potent inhibitor of the human11β-HSD1 with Ki of 2.3 nM and in vitro HEK293 EC50 of 15 nM, with minimal inhibitory activity toward the mouse enzyme (Ki=750 nM).

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