An 11β-HSD1 inhibitor
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AZD 8329

Item No. 45334

Technical Information
Formal Name
4-[5-(1,1-dimethylethyl)-4-[(tricyclo[3.3.1.13,7]dec-2-ylamino)carbonyl]-1H-pyrazol-1-yl]-benzoic acid
CAS Number
1048668-70-7
Molecular Formula
C25H31N3O3
Formula Weight
Purity
≥98%
A solid
SMILES
CC(C)(C(N(C(C=C1)=CC=C1C(O)=O)N=C2)=C2C(NC3[C@H]4C[C@H](C5)C[C@@H]3C[C@H]5C4)=O)C
InChi Code
InChI=1S/C25H31N3O3/c1-25(2,3)22-20(13-26-28(22)19-6-4-16(5-7-19)24(30)31)23(29)27-21-17-9-14-8-15(11-17)12-18(21)10-14/h4-7,13-15,17-18,21H,8-12H2,1-3H3,(H,27,29)(H,30,31)/t14-,15+,17-,18+,21?
InChi Key
XWBXJBSVYVJAMZ-HNDAYGKNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    AZD 8329 is an inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1; IC50 = 9 nM for the human enzyme).1 It is selective for 11β-HSD1 over 11β-HSD2 and 17β-HSD1 (IC50s = >30 µM for both), and over 17β-HSD3 with less than 5% inhibition at 10 µM. AZD 8329 (50 mg/kg per day) prevents impairments in cardiac function in a minipig model of myocardial infarction.2 Repeated oral administration of AZD 8329 over seven days induces tachyphylaxis in rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Scott, J.S., de Schoolmeester, J., Kilgour, E., et al. Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: The discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329). J. Med. Chem. 55(22), 10136-10147 (2012).

    2. Al Disi, S., Ascione, R., Khan, S., et al. Pharmacological inhibition of hydroxysteroid 11-beta dehydrogenase type 1 (11-βHSD1) after myocardial infarction preserves cardiac function in a translational mini-pig model. Br. J. Pharmacol. (2025).

    3. Morentin Gutierrez, P., Gyte, A., de Schoolmeester, J., et al. Continuous inhibition of 11β-hydroxysteroid dehydrogenase type I in adipose tissue leads to tachyphylaxis in humans and rats but not in mice. Br. J. Pharmacol. 172(20), 4806-4816 (2015).