An 11β-HSD1 inhibitor
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INCB 13739

Item No. 40223

Technical Information
Formal Name
(3S)-1-[(3-chloro-2-methylphenyl)sulfonyl]-N-cyclohexyl-3-piperidinecarboxamide
CAS Number
872506-67-7
Molecular Formula
C19H27ClN2O3S
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: SolubleMethanol: Soluble
SMILES
ClC1=CC=CC(S(N2CCC[C@@H](C2)C(NC3CCCCC3)=O)(=O)=O)=C1C
InChi Code
InChI=1S/C19H27ClN2O3S/c1-14-17(20)10-5-11-18(14)26(24,25)22-12-6-7-15(13-22)19(23)21-16-8-3-2-4-9-16/h5,10-11,15-16H,2-4,6-9,12-13H2,1H3,(H,21,23)/t15-/m0/s1
InChi Key
ODRPEKCTTLECBX-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    INCB 13739 is an inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1; IC50 = 3.2 nM).1 It is greater than 1,000-fold selective for 11β-HSD1 over 11β-HSD2, the mineralocorticoid receptor, and the glucocorticoid receptor at 5 µM. INCB 13739 inhibits 11β-HSD1 activity in peripheral blood mononuclear cells (PBMCs; IC50 = 1.1 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, C., Xu, M., He, C., et alDiscovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach. Bioorg. Med. Chem. Lett. 69:128782, (2022).