| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Androgen receptor (AR); MK-2866 (GTx-024) showed high AR binding affinity with Ki = 3.8 ± 0.5 nM (determined by competitive radioligand binding assay using ³H-mibolerone). [1]
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| ln Vitro |
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. MK-2866 (GTx-024) bound to AR with high affinity (Ki = 3.8 ± 0.5 nM). [1] In cotransfection assays using CV-1 cells co-transfected with human AR expression vector, luciferase reporter vector, and control β-galactosidase vector, MK-2866 (GTx-024) at a single concentration of 100 nM induced AR-mediated transcriptional activation to a level comparable to that induced by 1 nM dihydrotestosterone (DHT), indicating full agonist activity with no apparent difference from other cyano/nitro-substituted SARMs. [1] |
| ln 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.
MK-2866 (GTx-024) exhibited potent in vivo anabolic and androgenic activity in castrated male rats after 14 days of daily subcutaneous administration. [1] Dose-response analysis revealed ED50 values of 0.12 ± 0.05 mg/day for prostate, 0.39 ± 0.15 mg/day for seminal vesicles, and 0.03 ± 0.01 mg/day for levator ani muscle. [1] The maximum pharmacological effects (Emax) as percentage of intact control were: prostate 51.1 ± 4.2%, seminal vesicles 98.0 ± 13.2%, and levator ani muscle 136.3 ± 3.5%. [1] Relative potency in levator ani muscle was 4.41 compared to testosterone propionate (TP), and relative efficacy was 1.31, exceeding the anabolic activity of TP. [1] Efficacious and selective anabolic activity was observed at dose rates as low as 0.03 mg/day. [1] |
| Enzyme Assay |
The AR binding affinity was determined using an in vitro competitive radioligand binding assay. Rat cytosol was incubated with increasing concentrations (10⁻² to 5000 nM) of each ligand, a saturating concentration of ³H-mibolerone (1 nM), and 1000 nM triamcinolone acetonide to prevent interaction with progesterone receptors. Incubation was carried out at 4°C for 18 hours. Free and bound ³H-mibolerone were separated using the hydroxyapatite method. IC50 values were determined by nonlinear regression analysis, and the apparent equilibrium dissociation constant (Ki) was calculated using the equation Ki = Kd × IC50 / (Kd + L), where Kd is the dissociation constant of ³H-mibolerone (0.19 ± 0.01 nM) and L is the concentration of ³H-mibolerone used (1 nM). [1]
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| Cell Assay |
The transcriptional activity of MK-2866 (GTx-024) was measured using a cotransfection assay in CV-1 cells. CV-1 cells were co-transfected with a human androgen receptor expression vector, a luciferase reporter vector, and a control β-galactosidase vector. Transcriptional activation was assayed using a single concentration (100 nM) of the ligand and expressed as a percentage of that induced by 1 nM dihydrotestosterone. [1]
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| Animal Protocol |
Dissolved in DMSO, and diluted in saline; 1 mg/kg; s.c. administration Immature castrated male Sprague-Dawley rats
For in vivo pharmacodynamic studies: Immature male Sprague-Dawley rats (180-220 g) were castrated and randomly distributed into groups of five animals. MK-2866 (GTx-024) was administered via daily subcutaneous injection for 14 days at increasing doses (0.03, 0.1, 0.3, 0.5, 0.75, 1 mg/day). After 14 days, ventral prostates, seminal vesicles, and levator ani muscles were removed and weighed. Organ weights were normalized to body weight and compared with intact and castrated controls. [1] For pharmacokinetic studies: Immature male Sprague-Dawley rats (approximately 250 g) were implanted with a jugular vein catheter one day before dosing. MK-2866 (GTx-024) was dissolved in a vehicle consisting of 5% DMSO and 95% PEG 300 and administered as a single intravenous bolus dose at 10 mg/kg via the jugular vein. Blood samples (250 μl) were collected via the jugular vein at predetermined time intervals. Plasma was separated by centrifugation and stored at -20°C until analysis. [1] |
| ADME/Pharmacokinetics |
Pharmacokinetic parameters of MK-2866 (GTx-024) after a single intravenous dose (10 mg/kg) in male rats: terminal half-life (t1/2) = 6.0 h; plasma clearance (CL) = 1.4 ± 0.3 ml/min/kg; volume of distribution at steady state (Vss) = 635 ± 84 ml/kg; area under the plasma concentration-time curve from 0 to infinity (AUC∞) = 127 ± 27 μg·h/ml; mean residence time (MRT) = 475 ± 46 min. [1]
MK-2866 (GTx-024) showed the slowest clearance among the tested cyano/nitro-substituted SARMs, resulting in the highest systemic exposure. [1] |
| 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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| Additional Infomation |
Enobosarm has been used in clinical trials investigating the treatment of stress urinary incontinence and triple-negative breast cancer. Enobosarm is a nonsteroidal anti-inflammatory drug with anabolic activity. The selective androgen receptor modulator (SARM) GTx-024 has a mechanism of action similar to testosterone, thereby promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. By mimicking the effects of testosterone, this drug may increase lean body mass, thereby improving muscle atrophy in the hypermetabolic state of cancer cachexia.
MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with promising clinical potential for treating androgen deficiency-related disorders such as male hypogonadism, osteoporosis, muscle-wasting diseases, and for use in contraception. [1] The compound demonstrated tissue-selective activity, with full maintenance of seminal vesicle weight (98.0% of intact control) and supra-maximal anabolic effect on levator ani muscle (136.3% of intact control) at higher doses, while prostate weight was restored to 51.1% of intact control. [1] Relative potency in anabolic tissue (levator ani) was 4.41 times that of testosterone propionate, indicating high potency. [1] |
| Molecular Formula |
C19H14F3N3O3
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|---|---|---|
| Molecular Weight |
389.33
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| Exact Mass |
389.098
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| CAS # |
841205-47-8
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| Related CAS # |
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| PubChem CID |
11326715
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
632.3±55.0 °C at 760 mmHg
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| Flash Point |
336.2±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.578
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| LogP |
4.83
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
658
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@](COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
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| InChi Key |
JNGVJMBLXIUVRD-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C19H14F3N3O3/c1-18(27,11-28-15-6-2-12(9-23)3-7-15)17(26)25-14-5-4-13(10-24)16(8-14)19(20,21)22/h2-8,27H,11H2,1H3,(H,25,26)/t18-/m0/s1
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| Chemical Name |
(2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.42 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 :78 mg/mL (200.3 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5685 mL | 12.8426 mL | 25.6852 mL | |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.1370 mL | |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
'A Phase IIa Randomized, Placebo-Controlled, Parallel Group, Clinical Trial to Study the Efficacy and Safety of MK-2866 in Women with Moderate to Severe Chronic Obstructive Pulmonary Disease Participating in Pulmonary Rehabilitation'
CTID: null
Phase: Phase 2 Status: Prematurely Ended
Date: 2009-12-02
Products are for research use only; We do not sell to patients
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