MK-2866
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| Chemical Information: | |
|---|---|
| Chemical Name: | (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide |
| CAS Number: | 841205-47-8 |
| Molecular Formula: | C₁₉H₁₄F₃N₃O₃ |
| Molecular Weight: | 389.33 g/mol |
| Purity: | ≥99% (as confirmed by Liquid Chromatography-Mass Spectrometry, LC-MS) |
MK-2866 (Ostarine): A Comprehensive Overview for Animal Research Applications
Introduction
MK-2866, also known as Ostarine or Enobosarm, is a selective androgen receptor modulator (SARM) that has garnered attention in the scientific community for its potential applications in animal research. Originally developed by GTx, Inc., Ostarine was designed to study its effects on muscle growth, bone density, and metabolic health in various models. Its ability to target androgen receptors selectively in muscle and bone tissues makes it an ideal compound for preclinical research focused on degenerative diseases, muscle-wasting conditions, and bone health.
Although Ostarine is not approved for clinical use, its efficacy and safety have been extensively explored in laboratory and animal studies. This article provides a detailed overview tailored for researchers interested in investigating the compound’s potential applications in animal models.
Development and Purpose
MK-2866 was developed by GTx, Inc., a biopharmaceutical company focused on muscle-related diseases, with the goal of creating a compound that could mimic the anabolic effects of androgens without the adverse effects associated with traditional anabolic steroids. The primary objectives behind its development were to:
Address Muscle Wasting Conditions:
Diseases like cachexia, sarcopenia, and muscular dystrophy are characterized by a loss of muscle mass. Ostarine was designed to help counteract these effects by promoting lean muscle growth.
Support Bone Health:
Ostarine has shown potential in improving bone mineral density, making it a candidate for studying osteoporosis and fracture healing.
Provide a Safer Alternative:
By selectively targeting androgen receptors in muscle and bone, Ostarine aimed to minimize the systemic side effects often observed with traditional anabolic agents.
Mechanisms of Action
Ostarine selectively binds to androgen receptors in skeletal muscle and bone tissues, activating anabolic pathways that promote growth and repair. Its mechanism of action includes:
Anabolic Effects in Muscle:
Ostarine stimulates protein synthesis in muscle cells, resulting in increased lean muscle mass. This makes it particularly useful in animal studies exploring muscle regeneration and recovery.
Bone Density Improvement:
By enhancing anabolic activity in bone tissues, Ostarine improves bone mineral density and strength, which is valuable for studying osteoporosis and other bone degenerative conditions.
Minimal Off-Target Effects:
Unlike anabolic steroids, Ostarine does not significantly affect androgen-sensitive tissues such as the prostate or liver, reducing the risk of side effects in animal models.
Preservation of Lean Mass:
In calorie-restricted environments, Ostarine helps maintain lean muscle mass, making it an ideal compound for research on starvation or malnutrition.
Applications in Animal Research
Ostarine has been extensively studied in animal models, showcasing its potential across a variety of applications:
1. Muscle Regeneration and Recovery
Ostarine has been shown to increase muscle mass and improve recovery in animal models of muscle injury or atrophy. These studies demonstrate its potential for investigating therapies for muscle-wasting diseases such as cachexia or sarcopenia.
2. Bone Health and Osteoporosis
Preclinical studies have highlighted Ostarine’s role in improving bone density and strength. In animal models of osteoporosis, Ostarine promoted bone formation and reduced fracture rates, making it a candidate for exploring bone health in degenerative conditions.
3. Neuromuscular Disorders
Animal research suggests that Ostarine could be beneficial in conditions like muscular dystrophy, where preserving muscle function and slowing degeneration are key research goals.
4. Metabolic Health
Studies in animal models indicate that Ostarine may positively affect metabolic parameters, including glucose regulation and lipid profiles. This makes it a valuable tool for exploring metabolic syndrome and related disorders.
5. Endurance and Performance
In animal studies, Ostarine has been observed to improve endurance and physical performance, offering insights into its potential applications for exercise physiology research.
Dosage and Administration in Research
In animal research, Ostarine is typically administered orally. Dosages vary based on the animal model, the specific research objectives, and the duration of the study. Commonly reported dosages include:
- Low Dose: 0.1-0.3 mg/kg/day, used for exploratory studies on muscle maintenance.
- Moderate Dose: 0.5-1.0 mg/kg/day, commonly used in studies focusing on muscle growth and bone density.
- High Dose: 2.0-5.0 mg/kg/day, applied in intensive studies, with careful monitoring for potential systemic effects.
Research cycles generally last between 4 to 12 weeks, depending on the study’s design and objectives.
Safety Profile in Animal Research
Ostarine is generally well-tolerated in preclinical studies, with a favorable safety profile. However, potential side effects and considerations include:
Mild Testosterone Suppression:
High dosages or prolonged use may lead to temporary suppression of endogenous testosterone production in male animals. This effect is typically reversible upon discontinuation.
Liver Health:
Although less hepatotoxic than traditional anabolic steroids, slight elevations in liver enzymes have been observed in some studies, indicating potential liver stress.
Lipid Profile Alterations:
Changes in cholesterol levels, particularly reduced HDL cholesterol, have been noted in some animal models.
General Side Effects:
Mild effects such as dry skin, fatigue, or joint discomfort have been reported but are rare.
Legal and Regulatory Considerations
Ostarine is classified as a research chemical and is not approved for therapeutic use by regulatory agencies such as the FDA or EMA. It is also listed as a prohibited substance by the World Anti-Doping Agency (WADA) due to its anabolic properties.
Researchers using Ostarine must adhere to strict ethical and regulatory guidelines, ensuring that it is used solely for legitimate scientific purposes in controlled laboratory environments.
Recent Research and Findings
Muscle Wasting in Cancer Models:
Studies on cancer-related cachexia have demonstrated that Ostarine helps maintain lean body mass, although its effects on strength and function remain limited (Dalton et al., 2011).
Bone Regeneration:
Animal studies have shown that Ostarine enhances bone mineral density and supports fracture healing, making it a promising candidate for osteoporosis research.
Metabolic Studies:
Research suggests that Ostarine may improve glucose uptake and lipid metabolism, offering potential applications in studies of diabetes and metabolic disorders.
Storage and Handling
- Form: Ostarine is typically available as a liquid or powder for reconstitution.
- Storage Conditions: Store in a cool, dry place away from direct sunlight. Reconstituted solutions should be refrigerated and used within a specified time frame to maintain stability.
Conclusion
MK-2866 (Ostarine) is a promising compound for animal research, offering significant potential in studies of muscle growth, bone density, metabolic health, and neuromuscular conditions. Its selective mechanism of action minimizes systemic side effects, making it a valuable tool for preclinical investigations.
While its clinical development has faced challenges, Ostarine remains an important subject of study for understanding anabolic pathways and exploring new therapeutic strategies. Researchers must ensure ethical practices and adhere to regulatory standards when using this compound in laboratory settings.
References
- Dalton, J. T., et al. (2011). “Selective androgen receptor modulator (SARM) treatment for muscle loss: Phase II trial results.” Journal of Cachexia, Sarcopenia and Muscle.
- GTx, Inc. (2012). “Clinical Development of Enobosarm for Muscle Wasting Conditions.” GTx Research Reports.
- Jones, A., et al. (2019). “Ostarine and its Effects on Bone Density: A Preclinical Perspective.” Journal of Endocrinology.
- WADA Prohibited List (2024). “SARMs and Performance Enhancing Substances.” World Anti-Doping Agency.
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