Acetamoren
[CAS# 950841-87-9]

Identification

• Classification: API >> Hormone and endocrine-regulating drugs
• Name: Acetamoren
• Synonyms: MK-777; ibutamoren; Propanamide,2-(acetylamino)-N-[(1R)-2-[1,2-dihydro-1-(methylsulfonyl)spiro[3H-indole-3,4'-piperidin]-1'-yl]-2-oxo-1-[(phenylmethoxy)methyl]ethyl]-2-methyl-
• Molecular Formula: C₂₉H₃₈N₄O₆S
• Molecular Weight: 570.70
• CAS Registry Number: 950841-87-9
• EC Number: 200-001-7
• SMILES: C12=CC=CC=C1C3(CN2[S](C)(=O)=O)CCN(CC3)C(C(COCC4=CC=CC=C4)NC(C(C)(C)NC(C)=O)=O)=O

Properties

• Density: 1.318±0.10 g/cm³ (25 ºC, 760 Torr)
• Melting point: 174.0?-181.0? ºC

Discovory and Applicatios

Acetamoren, also known by its research code MK-677 or Ibutamoren, is a non-peptidic agonist of the ghrelin receptor and a potent stimulator of growth hormone (GH) secretion. It was developed in the 1990s with the aim of providing an orally active compound that mimics the GH-stimulating effects of endogenous ghrelin without requiring injection. Acetamoren acts by binding to the growth hormone secretagogue receptor (GHS-R1a), leading to increased levels of both GH and insulin-like growth factor 1 (IGF-1) in the circulation. This mechanism has made it a compound of considerable interest in the treatment of GH deficiency and muscle wasting disorders.

The compound was initially studied for its potential to treat GH deficiency in both children and adults. Clinical trials demonstrated that once-daily oral administration of Acetamoren resulted in a sustained increase in serum GH and IGF-1 levels, comparable to those achieved through recombinant GH injections. This property offered the promise of a more convenient alternative to traditional GH therapies. Despite its efficacy, development for this indication was not fully pursued due to regulatory and safety considerations, particularly in pediatric populations.

Another promising application of Acetamoren has been in the prevention of muscle atrophy and frailty in elderly patients. Age-related sarcopenia, characterized by the progressive loss of muscle mass and function, is a growing concern in aging populations. Acetamoren’s ability to stimulate GH and IGF-1 suggests a potential role in improving muscle strength and physical performance in older individuals. Several clinical studies have shown increases in lean body mass following Acetamoren treatment, although improvements in functional outcomes such as strength or endurance have been less consistently observed.

Beyond musculoskeletal health, Acetamoren has been evaluated for its potential benefits in metabolic disorders. Because ghrelin and GH both influence appetite and energy homeostasis, Acetamoren has been explored as a possible treatment for obesity and cachexia. However, its appetite-stimulating effects, while useful in undernourished individuals, present challenges in populations prone to weight gain. In some studies, subjects reported increased appetite and body weight, reflecting Acetamoren’s dual action on both anabolic and orexigenic pathways.

Preclinical research has also investigated the effects of Acetamoren in models of bone density loss and wound healing. In rodent studies, chronic administration of the compound was associated with increases in bone mineral density and enhanced healing of soft tissue injuries, effects attributed to the elevated IGF-1 levels induced by the drug. These findings suggest that Acetamoren may have broader regenerative properties beyond muscle anabolism.

Despite its potential, Acetamoren remains an investigational compound. It has not been approved by regulatory agencies for therapeutic use, and its long-term safety profile has not been fully established. Nonetheless, it continues to be studied in clinical settings and has garnered attention in sports and bodybuilding communities due to its anabolic-like effects. This off-label use has raised concerns about misuse and prompted efforts to monitor its distribution and availability, especially via online sources.

In summary, Acetamoren represents a significant development in the field of GH secretagogues. Its oral bioavailability, prolonged action, and ability to elevate GH and IGF-1 levels make it an attractive candidate for treating conditions associated with GH deficiency and muscle loss. Ongoing research will determine whether its therapeutic benefits can be realized safely and effectively in broader patient populations.