LGD-2226 is a selective and orally active androgen receptor modulator (EC50: 0.2 nM, Ki: 1.5 nM for the human androgen receptor). LGD-2226 can be used for muscle wasting, osteoporosis, and sexual dysfunction.

Androgen receptor:(EC50)0.2 nM, Androgen receptor:(ki)1.5 nM

LGD-2226 occupies the same binding pocket as dihydrotestosterone (DHT), the protein backbone is superposable to that observed with DHT. The trifluoroethyl groups of LGD-2226 occupy the same space in the receptor as the C and D rings of the steroid. GLN711 forms an additional hydrogen bond with the quinolone NH of LGD-2226. Just like the carbonyl group of DHT, the quinolone carbonyl forms hydrogen bond interactions with GLN711 and ARG752 [1].

LGD-2226 has weak trophic effects on the prostate. LGD-2226 (100 mg/kg) treatment, is required to maintain prostate weight at intact levels. LGD-2226 (1-100 mg/kg; p.o.; daily; for 2 weeks; adult oORDX rats) has a pronounced effect on the levator ani muscle, maintaining the muscle weight at the eugonadal levels at an approximate 3 mg/kg dose. These data clearly show the tissue selectivity of LGD-2226[1].