MK-0773

• CAT Number: I004282
• CAS Number: 606101-58-0
• Molecular Formula: C27H34FN5O2
• Molecular Weight: 479.59
• Purity: ≥95%
• Target: Androgen Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 6.6 nM [1]

MK-0773(PF05314882), one of selective androgen receptor modulators (SARMs), is a 4-aza-steroid that exhibited tissue selectivity in humans (IC50= 6.6 nM).IC50 Value: 6.6 nM [1]Target: Androgen receptorin vitro: 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 it binds to serum proteins. The affinity of MK-0773 for AR across species was evaluated using COS cells transfected with AR, and IC50 values were very similar in four species (rat, 0.50 nM; dog, 0.55 nM; rhesus, 0.45 nM; human, 0.65 nM) [1].in vivo: MK-0773 was dosed subcutaneously for 24 days in the OVX rat model (6 and 80 mg/kg) and produced plasma exposures over 24 h of 6.6 and 62 μM·h. This treatment produced exposure-related stimulatory effects on cortical BFR and LBM. The maximal anabolic effects of MK-0773 were equivalent to the SARM TFM-4AS-1 and 80% of 3 mg/kg DHT [1]. 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].Clinical trial: Safety, Tolerability and Efficacy of MK-0773 in Healthy Postmenopausal Women. Phase 1

Reference

1:Identification of selected in vitro generated phase-I metabolites of the steroidal selective androgen receptor modulator MK-0773 for doping control purposes. Lagojda A, Kuehne D, Krug O, Thomas A, Wigger T, Karst U, Schänzer W, Thevis M.Eur J Mass Spectrom (Chichester). 2016;22(2):49-59. doi: 10.1255/ejms.1415. PMID: 27419898 2: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. Papanicolaou DA, Ather SN, Zhu H, Zhou Y, Lutkiewicz J, Scott BB, Chandler J.J Nutr Health Aging. 2013;17(6):533-43. doi: 10.1007/s12603-013-0335-x. PMID: 23732550 3: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. Schmidt A, Kimmel DB, Bai C, Scafonas A, Rutledge S, Vogel RL, McElwee-Witmer S, Chen F, Nantermet PV, Kasparcova V, Leu CT, Zhang HZ, Duggan ME, Gentile MA, Hodor P, Pennypacker B, Masarachia P, Opas EE, Adamski SA, Cusick TE, Wang J, Mitchell HJ, Kim Y, Prueksaritanont T, Perkins JJ, Meissner RS, Hartman GD, Freedman LP, Harada S, Ray WJ.J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31. PMID: 20356837 Free PMC Article