A CYP17A1 inhibitor
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Abiraterone Acetate

Item No. 15148

Technical Information
Formal Name
(3β)-17-(3-pyridinyl)-androsta-5,16-dien-3-ol, acetate ester
CAS Number
154229-18-2
Synonyms
  • CB-7630
Molecular Formula
C26H33NO2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 16 mg/mlDMSO: 2 mg/mlEthanol: 16 mg/mlEthanol:PBS (pH 7.2)(1:2): 0.3 mg/ml
λmax
254 nm
SMILES
C[C@]12C(C[C@@H](OC(C)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC=C4C5=CC=CN=C5
InChi Code
InChI=1S/C26H33NO2/c1-17(28)29-20-10-12-25(2)19(15-20)6-7-21-23-9-8-22(18-5-4-14-27-16-18)26(23,3)13-11-24(21)25/h4-6,8,14,16,20-21,23-24H,7,9-13,15H2,1-3H3/t20-,21-,23-,24-,25-,26+/m0/s1
InChi Key
UVIQSJCZCSLXRZ-UBUQANBQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Abiraterone acetate is an inhibitor of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 17 and 18 nM for inhibition of C17,20-lyase and 17α-hydroxylase activities, respectively).1 It is also a prodrug form of abiraterone (Item No. 9002768).2 Abiraterone acetate reduces plasma testosterone levels, increases plasma luteinizing hormone levels, and reduces ventral prostate, seminal vesicle, testis, and kidney weight in mice when administered at doses of 0.1 and 0.5 mmol/kg per day. It also reduces severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral load in the culture supernatant of infected Vero E6 cells (EC90 = 8.4 μM) and is active in a plaque reduction assay (EC50 = 1.94 μM).3 Formulations containing abiraterone acetate have been used in combination therapy for the treatment of metastatic castration-resistant prostate cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Potter, G.A., Barrie, S.E., Jarman, M., et alNovel steroidal inhibitors of human cytochrome P45017α (17α-hydroxylase-C17,20-lyase): Potential agents for the treatment of prostatic cancer. J. Med. Chem. 38(13), 2463-2471 (1995).

    2. Barrie, S.E., Potter, G.A., Goddard, P.M., et alPharmacology of novel steroidal inhibitors of cytochrome P45017α (17α-hydroxylase/C17-20 lyase). J. Steroid Biochem. Mol. Biol. 50(5-6), 267-273 (1994).

    3. Yuan, S., Chan, J.F.W., Chik, K.K.H., et alDiscovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system. Pharmacol. Res. 159, 104960 (2020).