Catalog No.S1174 Synonyms: Enobosarm, ostarine
Molecular Weight(MW): 389.33
MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
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|Description||MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.|
|Features||The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.|
Ostarine at the concentration of 10 nM modulates the transcriptional activity of AR in CV-1 cells cotransfected with a human AR expression vector, a luciferase reporter vector, and a control β-galactosidase vector, with 94%-100% relative activity of the transcriptional activation observed for 1 nM DHT.  
|In vivo||After intravenous administration of Ostarine at a single dose of 10 mg/kg, plasma concentration of Ostarine declines slowly, exhibiting a longer terminal half-life of 6.0 hours, as compared to that of other related cyano/nitro group-substituted SARMs with terminal halflives of 2.6-4.0 hours. Ostarine exhibits significantly androgenic and anabolic activity by stimulating the growth of prostate, seminal vesicles, and levator ani muscle when administered in castrated male rats; Ostarine is more potent than other cyano/nitro group-substituted SARMs. Ostarine restores the weight of the prostate to 39.2%, and seminal vesicle 78.8%, and stimulates the growth of levator ani muscle to a greater extent of 141.9% as compared with that of androgenic organs. Ostarine exhibits the highest in vivo androgenic and anabolic activity of any AR nonsteroidal agonist examined to date, with ED50 values of 0.12, 0.39 and 0.03 mg/day in prostate, seminal vesicles, and levator ani muscle, respectively, being 4 times as potent as testosterone propionate (TP) in levator ani muscle. At low dose of 0.03 mg/day, Ostarine is sufficient to exert efficacious and selective activity in anabolic tissues. |
|In vitro||DMSO||78 mg/mL (200.34 mM)|
|Ethanol||78 mg/mL (200.34 mM)|
|In vivo||1% DMSO+30% polyethylene glycol+1% Tween 80||5 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02971761||Not yet recruiting||Androgen Receptor Positive|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma||City of Hope Medical Center|National Cancer Institute (NCI)||January 2017||Phase 2|
|NCT02746328||Not yet recruiting||ER+ and AR+ Breast Cancer||GTx|Martin Performance||April 2016||Phase 2|
|NCT02658448||Recruiting||Stress Urinary Incontinence||GTx||January 2016||Phase 2|
|NCT02463032||Recruiting||ER+ and AR+ Breast Cancer||GTx||August 2015||Phase 2|
|NCT02368691||Recruiting||Triple Negative Breast Cancer||GTx||June 2015||Phase 2|
|NCT01616758||Active, not recruiting||Metastatic Breast Cancer||GTx||April 2013||Phase 2|
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