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Selective androgen receptor modulator
LG121071
Другие языки:

    LG121071

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    LG121071
    LG-121071.svg
    Clinical data
    Other names LG-121071; LGD-121071
    Identifiers
    • 6-Ethyl-4-(trifluoromethyl)-1H,2H,6H,7H,8H,9H-pyrido[3,2-g]quinolin-2-one
    CAS Number
    PubChem CID
    ChemSpider
    ChEMBL
    Chemical and physical data
    Formula C15H15F3N2O
    Molar mass 296.293 g·mol−1
    3D model (JSmol)
    • CCC1CCNC2=C1C=C3C(=CC(=O)NC3=C2)C(F)(F)F
    • InChI=1S/C15H15F3N2O/c1-2-8-3-4-19-12-7-13-10(5-9(8)12)11(15(16,17)18)6-14(21)20-13/h5-8,19H,2-4H2,1H3,(H,20,21)
    • Key:SZPPQFARTYXRKU-UHFFFAOYSA-N

    LG121071 (or LGD-121071) is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered. It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine). The drug acts as a high-affinity full agonist of the androgen receptor (AR) (Ki = 17 nM), with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT). Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues (nor aromatized into estrogenic metabolites), and for this reason, show tissue-selective androgenic effects. In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids.

    The in vitro metabolism of LG121071 has been characterized in anticipation of its possible use as a doping agent.

    See also



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