MK-0773 - CAS 606101-58-0
Catalog number: 606101-58-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H34FN5O2
Molecular Weight:
479.59
COA:
Inquire
Targets:
Androgen Receptor
Description:
MK-0773 is a selective androgen receptor modulator for the prevention and treatment of muscle wasting associated with cancer. It designed to improve muscle function while minimizing effects on other tissues, inducing increases in lean body mass. It is a 4-aza-steroid that exhibited tissue selectivity in humans with IC50 value of 6.6 nM. It is useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture and so on. It was developed by Merck Sharp & Dohme and was in clinic phase 2 trials, but now it is terminated.
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Purity:
98%
Appearance:
Light yellow to yellow solid
Synonyms:
PF05314882;PF-05314882;N-(3H-Imidazo[4,5-b]pyridin-2-ylmethyl)-2-fluoro-4-methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide;(1S,3aS,3bS,5aR,9aS,9bS,11aS)-8-fluoro-N-(1H-imidazo[4,5-b]pyridin-2-ylmethyl)-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,9
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
MK-0773 is designed to improve muscle function while minimizing effects on other tissues, inducing increases in lean body mass. It is useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which
Quality Standard:
In-house standard
Quantity:
Grams to Kilograms
Boiling Point:
754.2±60.0 °C | Condition: Press: 760 Torr
Density:
1.31±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
GBEUKTWTUSPHEE-JWJWXJQQSA-N
InChI:
InChI=1S/C27H34FN5O2/c1-26-11-10-17-15(6-9-21-27(17,2)13-19(28)25(35)33(21)3)16(26)7-8-18(26)24(34)30-14-22-31-20-5-4-12-29-23(20)32-22/h4-5,12-13,15-18,21H,6-11,14H2,1-3H3,(H,30,34)(H,29,31,32)/t15-,16-,17-,18+,21+,26-,27+/m0/s1
Canonical SMILES:
CC12CCC3C(C1CCC2C(=O)NCC4=NC5=C(N4)C=CC=N5)CCC6C3(C=C(C(=O)N6C)F)C
Current Developer:
MK-0773 was developed by Merck Sharp & Dohme and was in clinic phase 2 trials, but now it is terminated.
1.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 A1, 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 J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31.
Selective androgen receptor modulators (SARMs) are androgen receptor (AR) ligands that induce anabolism while having reduced effects in reproductive tissues. In various experimental contexts SARMs fully activate, partially activate, or even antagonize the AR, but how these complex activities translate into tissue selectivity is not known. Here, we probed receptor function using >1000 synthetic AR ligands. These compounds produced a spectrum of activities in each assay ranging from 0 to 100% of maximal response. By testing different classes of compounds in ovariectomized rats, we established that ligands that transactivated a model promoter 40-80% of an agonist, recruited the coactivator GRIP-1 <15%, and stabilized the N-/C-terminal interdomain interaction <7% induced bone formation with reduced effects in the uterus and in sebaceous glands. Using these criteria, multiple SARMs were synthesized including MK-0773, a 4-aza-steroid that exhibited tissue selectivity in humans.
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 DA1, 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.
BACKGROUND: Sarcopenia, the age-related loss of muscle mass [defined as appendicular LBM/Height2 (aLBM/ht2) below peak value by>1SD], strength and function, is a major contributing factor to frailty in the elderly. MK-0773 is a selective androgen receptor modulator designed to improve muscle function while minimizing effects on other tissues.
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CAS 606101-58-0 MK-0773

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