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MK-677

GH Secretagogue
IbutamorenIbutamoren MesylateL-163191MK677

Overview

MK-677, also known as Ibutamoren, Ibutamoren Mesylate, or L-163191, is a non-peptide growth hormone secretagogue that mimics the action of ghrelin, a hormone that stimulates growth hormone (GH) release. It was originally developed by Merck & Co. and is structurally distinct from peptide-based secretagogues. The compound is synthesized through a series of chemical reactions that result in a mesylate salt form, enhancing its stability and solubility. Researchers have primarily investigated MK-677 for its potential to increase growth hormone and insulin-like growth factor 1 (IGF-1) levels in humans. Studies have shown that it can promote lean body mass and improve bone density, making it a candidate for conditions such as growth hormone deficiency, muscle wasting, and osteoporosis. Additionally, it has been explored for its effects on sleep quality and cognitive function. MK-677 acts by binding to the ghrelin receptor (GHSR), which is a G-protein-coupled receptor. This interaction stimulates the pituitary gland to release growth hormone, thereby increasing circulating levels of GH and IGF-1. Unlike direct GH administration, MK-677 does not suppress the body's natural GH production. The pharmacokinetic profile of MK-677 indicates a half-life of approximately 4 to 6 hours when administered orally, allowing for once-daily dosing. It is well-absorbed with high oral bioavailability, and its effects on GH secretion can last for up to 24 hours. Current research on MK-677 is ongoing, with several clinical trials examining its efficacy and safety in various populations. It is not approved by major regulatory agencies for medical use, and its sale is often limited to research purposes. The compound remains under investigation for its therapeutic potential and long-term effects.

Mechanism of Action

MK-677 functions by binding to the growth hormone secretagogue receptor (GHSR), which is the receptor for ghrelin. This binding stimulates the release of growth hormone from the pituitary gland, leading to increased levels of growth hormone and IGF-1 in the bloodstream. The activation of GHSR also influences appetite and energy homeostasis.

Molecular Data

FormulaC28H40N4O8S2
Molecular Weight624.8 g/mol
CAS Number159752-10-0
PubChem CID6450830

Half-Life

IntranasalNot applicable
Oral~4 to 6 hours

MK-677 is primarily administered orally due to its high bioavailability and prolonged effect on GH levels.

Storage

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Solubility

MK-677 is soluble in DMSO and ethanol but has limited solubility in water.

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA for any medical use. Not scheduled by the DEA.

🇦🇺AU

Not approved by the TGA. Considered a Schedule 4 substance, requiring prescription for therapeutic use.

🇬🇧UK

Not approved by the MHRA for medical use. Sale for research purposes only.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

10 Research Publications

Hepatotoxicity induced by MK-677.

Case Report

BMJ case reports · 2025

Researchers studied the effects of MK-677, a supplement that stimulates growth hormone release, and found that it can lead to liver damage in some individuals. In a case involving a healthy man in his 30s, liver function tests showed abnormalities after two months of use, which returned to normal after he stopped taking the supplement.

  • MK-677 is increasingly used as a performance-enhancing supplement.
  • The case involved a healthy man who developed liver function abnormalities after two months of MK-677 use.
  • Liver function tests normalized after discontinuing the supplement.
PubMed

LGD-4033 and MK-677 use impacts body composition, circulating biomarkers, and skeletal muscle androgenic hormone and receptor content: A case report.

Case Report

Experimental physiology · 2022

Researchers found that the combination of LGD-4033 and MK-677 led to increased body mass and changes in body composition, including gains in both lean and fat mass. However, this co-administration also negatively affected bone health and several important blood markers. The study highlights the need for more research on the health impacts of these substances among recreational users.

  • Co-administration of LGD-4033 and MK-677 increased body mass by 6% and lean mass by 3.1%.
  • Bone mineral content decreased by 3.6%, and several serum lipid markers showed significant increases.
  • Intramuscular androgen levels and strength improved, but free testosterone levels dropped by 85.7% during the study.
PubMed

Characterization of growth hormone secretagogue small molecule ibutamoren (MK-0677) and its possible metabolites in thoroughbred horses for doping control.

Unknown

Rapid communications in mass spectrometry : RCM · 2022

Researchers studied ibutamoren (MK-0677), a growth hormone secretagogue, in thoroughbred horses to understand its effects and metabolites after oral use. They found that ibutamoren can be detected in the body for up to 72 hours, with its metabolites remaining identifiable for up to 96 hours, which is important for monitoring potential doping in sports.

  • Researchers identified 22 metabolites of ibutamoren, including 17 phase I and 5 phase II metabolites.
  • The major metabolites of ibutamoren can be detected for up to 96 hours after administration.
  • Ibutamoren itself can persist in the system for up to 72 hours following a single dose.
PubMed

A GH Secretagogue Receptor Agonist (LUM-201) Elicits Greater GH Responses than Standard GH Secretagogues in Subjects of a Pediatric GH Deficiency Trial.

Human

Hormone research in paediatrics · 2022

Researchers found that LUM-201, an oral medication for pediatric growth hormone deficiency, produced significantly higher growth hormone responses compared to standard diagnostic tests in children. This suggests that LUM-201 could be a promising alternative to traditional injectable treatments for some patients.

  • LUM-201 elicited greater growth hormone responses than standard diagnostic tests like arginine and glucagon.
  • The difference in growth hormone responses was most pronounced in children with higher baseline IGF-I levels.
  • LUM-201 may offer a convenient oral treatment option for patients who respond well to its acute effects.
PubMed

Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males.

Review

Translational andrology and urology · 2020

Researchers reviewed the role of growth hormone secretagogues (GHS) as a potential treatment for men with low testosterone levels, known as hypogonadism. They found that while testosterone is the standard treatment, GHS may offer additional benefits for improving body composition and alleviating some symptoms associated with hypogonadism, although more research is needed to confirm their effectiveness.

  • Researchers observed that male hypogonadism is linked to obesity and metabolic syndrome, affecting overall health.
  • The review highlighted that growth hormone secretagogues, like sermorelin and ibutamoren, could improve body composition and reduce symptoms of hypogonadism.
  • However, the current lack of extensive clinical data limits understanding of how GHS can be effectively integrated into treatment for hypogonadal men.
PubMed

Effect of the Orally Active Growth Hormone Secretagogue MK-677 on Somatic Growth in Rats.

Animal

Yonsei medical journal · 2018

Researchers studied the effects of MK-677, a growth hormone secretagogue, on growth in rats. They found that while MK-677 increased growth hormone levels, it did not lead to significant growth in body size or related growth factors over six weeks of treatment.

  • MK-677 increased peak growth hormone levels by 1.8 times compared to baseline.
  • Despite the increase in growth hormone, there was no significant change in body growth or insulin-like growth factor levels.
  • The study noted changes in gene expression related to growth hormone regulation, suggesting a potential desensitization effect with prolonged MK-677 use.
PubMed

The Safety and Efficacy of Growth Hormone Secretagogues.

Review

Sexual medicine reviews · 2018

Researchers reviewed the safety and effectiveness of growth hormone secretagogues (GHSs), which stimulate the release of growth hormone in the body. They found that while GHSs may improve growth and lean body mass, more research is needed to fully understand their long-term safety and effects on health.

  • GHSs may enhance growth velocity in children and increase lean mass in individuals with obesity or wasting conditions.
  • The compounds are generally well tolerated, but there are concerns about their potential to increase blood glucose levels.
  • Long-term studies on the safety of GHSs, particularly regarding cancer risk, are still needed.
PubMed

MK-0677 (ibutamoren mesylate) for the treatment of patients recovering from hip fracture: a multicenter, randomized, placebo-controlled phase IIb study.

Human

Archives of gerontology and geriatrics · 2011

Researchers studied the effects of MK-0677 on elderly patients recovering from hip fractures. They found that while MK-0677 increased certain hormone levels, it did not significantly improve most measures of physical function, and there were safety concerns related to heart health.

  • Researchers observed a small increase in stair climbing power and gait speed in patients taking MK-0677 compared to those on placebo.
  • The study noted fewer falls among patients taking MK-0677, although this was not statistically significant.
  • Researchers found an increase in IGF-1 hormone levels in the MK-0677 group, but this was not linked to improved physical performance.
PubMed

Effects of oral administration of ibutamoren mesylate, a nonpeptide growth hormone secretagogue, on the growth hormone-insulin-like growth factor I axis in growth hormone-deficient children.

Human

Clinical pharmacology and therapeutics · 2001

Researchers studied the effects of ibutamoren mesylate, a growth hormone stimulator, in children with growth hormone deficiency. They found that short-term use of this compound increased levels of growth hormone and insulin-like growth factor I, which are important for growth.

  • Researchers observed a significant increase in peak serum growth hormone levels after treatment.
  • There was also a notable rise in insulin-like growth factor I levels, which is crucial for growth.
  • No adverse effects on other hormone levels or glucose were detected during the study.
PubMed

MK-677, an orally active growth hormone secretagogue, reverses diet-induced catabolism.

Human

The Journal of clinical endocrinology and metabolism · 1998

Researchers studied the effects of MK-677, a growth hormone secretagogue, on healthy volunteers undergoing caloric restriction. They found that MK-677 significantly improved nitrogen balance, indicating less protein loss compared to a placebo, suggesting potential benefits for individuals experiencing muscle wasting due to illness.

  • MK-677 improved nitrogen balance during caloric restriction, reversing diet-induced protein loss.
  • Participants taking MK-677 had higher levels of insulin-like growth factor-I (IGF-I) compared to those on placebo.
  • The study indicated that MK-677 was well tolerated with no significant adverse effects reported.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.