Ostarine (aslo known as Enobosarm, GTx024, MK2866, GTx-024, MK-2866) is a novel, potent and selective androgen receptor modulator (SARM) with potential antitumor activity. It inhibits ndrogen receptor with a Ki of 3.8 nM, and is tissue-selective for anabolic organs. MK-2866 is developed by GTx Inc and was designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. SARMs represent an emerging class of small molecule pharmacotherapeutics that have the potential to afford the important benefits of androgen therapy without the undesired side-effects. Many SARMs with demonstrated tissue-selective effects are currently in the early stages of development
理化性质和储存条件
| Molecular Weight (MW) | 389.33 |
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| Formula | C19H14F3N3O3 |
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| CAS No. | 841205-47-8 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 78 mg/mL (200.3 mM) |
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| Water: <1 mg/mL |
| Ethanol: 78 mg/mL (200.3 mM) |
| Solubility (In vivo) | 1% DMSO+30% polyethylene glycol+1% Tween 80: 78 mg/mL (200.3 mM) |
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| Synonyms | Enobosarm, ostarine; MK2866; GTX024; MK 2866; GTX 024; MK-2866; GTX-024 |
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实验参考方法
| In Vitro | In vitro activity: 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.
Kinase Assay: MK-2866 (aslo known as Enobosarm, GTx-024, Ostarine) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. MK-2866 is developed by GTx Inc and was designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. |
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| 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. |
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| Animal model | Immature castrated male Sprague-Dawley rats |
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| Formulation & Dosage | Dissolved in DMSO, and diluted in saline; 1 mg/kg; s.c. administration |
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| References | J Pharmacol Exp Ther. 2005 Oct;315(1):230-9; J Med Chem. 2011 Jun 9;54(11):3973-6. |
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