MK-0773

Short Summary : Selective androgen receptor modulators

Category : Endocrinology and Hormones|Androgen Receptor

Purity : 0.98

CAS Number : 606101-58-0

Formula : C27H34FN5O2

Molecular Weight : 479.59

SMILE : CC12CCC3C(C1CCC2C(=O)NCC4=NC5=C(N4)C=CC=N5)CCC6C3(C=C(C(=O)N6C)F)C

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : MK-0773Description:IC50: 6.6 nMSelective androgen receptor modulators (SARMs) are androgen receptor (AR) ligands that induce anabolism while having reduced effects in reproductive tissues. MK-0773(PF05314882), one of SARMs, is a 4-aza-steroid exhibiting tissue selectivity in human [1].In vitro: Previous study showed that the IC50 of MK-0773 binding to AR was increased 3.5-fold in the presence of 25% rat serum and 13-fold in the presence of 25% human serum, indicating that MK-0773 binds to serum proteins. In addition, the AR affinity of MK-0773 across species was evaluated using AR transfected COS cells, and it was found that IC50 values were very similar in four studied species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM) [1]. In vivo: MK-0773 was subcutaneously given to the OVX rat (6 and 80 mg/kg) for 24 days resulting in plasma exposures over 24 h of 6.6 and 62 μM?h. The MK-0773 treatment produced exposure-related stimulatory effects on cortical BFR and LBM. The maximal anabolic effects of MK-0773 were found to be equivalent to the SARM TFM-4AS-1 and ~80% of 3 mg/kg DHT. In summary, MK-0773 exhibits the profile of an anabolic SARM with limited effects on the sebaceous glands and reproductive tracts of OVX rats. [1]. Clinical trial: In a phase IIA clinical trial, participants receiving MK-0773 showed a statistically significant increase in LBM from baseline at Month 6 vs. placebo (p<0.001). Participants receiving both MK-0773 and placebo showed a statistically significant increase in strength from baseline to Month 6, but the mean difference between the two groups was not significant (p=0.269) [2].Reference:[1] Schmidt A, Kimmel DB, Bai C, Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology. J Biol Chem. 2010;285(22):17054-64.[2] Papanicolaou DA, Ather SN, Zhu H, A phase IIA randomized, placebo-controlled clinical trial to study the efficacy and safety of the selective androgen receptor modulator (SARM), MK-0773 in female participants with sarcopenia. J Nutr Health Aging. 2013;17(6):533-43.

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