Hexarelin
Hexarelin (Examorelin)
Potent Growth Hormone Secretagogue with Cardiac Benefits
What is Hexarelin?
Hexarelin is a synthetic hexapeptide and one of the most potent members of the growth hormone secretagogue (GHS) family. Structurally similar to GHRP-6 but modified for improved metabolic stability and receptor binding affinity, hexarelin produces GH pulses of greater magnitude than either GHRP-6 or GHRP-2 at equivalent molar doses. In preclinical studies comparing hexarelin directly to ghrelin, hexarelin demonstrated superior chemical stability and more potent GH-releasing activity, making it particularly useful as a research tool for studying the GH axis.
Hexarelin exerts its biological actions through two distinct receptor populations. The first is the growth hormone secretagogue receptor type 1a (GHS-R1a), the primary receptor mediating GH release from the pituitary and the same receptor targeted by ghrelin and other GHRPs. Activation of GHS-R1a by hexarelin triggers GH secretion with downstream increases in insulin-like growth factor 1 (IGF-1). The second receptor is CD36, a scavenger receptor expressed in cardiac tissue, macrophages, and adipose tissue. CD36 is the receptor through which hexarelin exerts its cardioprotective effects, which appear to be substantially independent of GH release. This dual-receptor engagement distinguishes hexarelin from most other GH secretagogues.
The cardiovascular research around hexarelin is among the most compelling in the GHS class. Multiple peer-reviewed studies have documented that hexarelin improves left ventricular function in ischemic heart failure models. Research published in Frontiers in Endocrinology demonstrated that hexarelin treatment in rats following experimental myocardial infarction increased stroke volume, cardiac output, and cardiac index while decreasing total peripheral resistance. Mechanistic studies identified that hexarelin's cardioprotection involves regulation of the interleukin-1 signaling pathway through GHS-R1a activation, as well as maintenance of normal calcium handling in cardiomyocytes during ischemia-reperfusion injury. These effects were observed even in GH-deficient models, confirming they are not secondary to GH elevation.
Hexarelin has also shown beneficial effects on lipid metabolism. Research using insulin-resistant mouse models (MKR mice) found that hexarelin treatment improved lipid aberrations and reduced fat accumulation, with effects that again appeared at least partly independent of its somatotropic activity. Hexarelin is not approved by the FDA for any clinical indication and is available only as a research compound.
Research Supply
Source high-purity Hexarelin for your research
Dosage Guide
Route: Subcutaneous injection, preferably in a fasted state to maximize GH pulse amplitude
Dosing Schedule
| Period | Dose |
|---|---|
| Entry level | 100 mcg, 1-2x daily (assess individual tolerance) |
| Standard research | 200 mcg, 2x daily (morning fasted + evening) |
| High dose | 400 mcg, 2x daily (maximum GH pulse; plateau occurs above ~2 mcg/kg) |
| Combined with GHRH analog | 100 mcg hexarelin + 100 mcg CJC-1295, 2x daily |
Reconstitution
Injection Volumes
| Dose | Volume | Syringe Units |
|---|---|---|
| 100 mcg | 0.05 mL | 5 units |
| 200 mcg | 0.10 mL | 10 units |
| 400 mcg | 0.20 mL | 20 units |
Cycling Protocol
6-8 weeks
4-8 weeks
Shorter cycles are recommended compared to other GHRPs due to hexarelin's higher potency and faster receptor desensitization
Administration Tips
- Inject in a fasted state -- elevated blood glucose and circulating fatty acids blunt GH secretion
- A saturation or plateau effect is observed above approximately 2 mcg/kg in humans -- higher doses do not produce proportionally larger GH pulses
- Desensitization of the GHS-R1a receptor occurs more readily with hexarelin than with some other secretagogues due to its high binding affinity
- Research protocols often include cycle breaks or rotation with lower-affinity secretagogues to maintain receptor sensitivity
- Monitor cortisol and prolactin in longer research protocols -- hexarelin elevates both more than ipamorelin
- Inject subcutaneously, avoiding the postprandial period for maximum effectiveness
Risks & Side Effects
Commonly Reported
Serious Risks
Promotion of tumor growth
Elevated GH and IGF-1 are mitogenic. Individuals with active malignancy or high cancer risk should not use hexarelin.
Receptor desensitization
Hexarelin's high potency can lead to tachyphylaxis with prolonged continuous use, diminishing GH response over time.
Worsening insulin resistance
GH is a counter-regulatory hormone that impairs insulin sensitivity, particularly at higher GH concentrations.
Carpal tunnel syndrome
Sustained IGF-1 elevation from prolonged use can cause progressive carpal tunnel syndrome.
Hypopituitarism risk
Theoretical risk with chronic very high-dose use based on continuous GHS-R1a suppression; not confirmed in clinical use.
Contraindications
- Active or prior malignancy (growth-promoting hormonal environment)
- Diabetes mellitus or clinically significant insulin resistance
- Pregnancy and lactation
- Active acromegaly or elevated baseline GH/IGF-1
- Pediatric use in individuals with open growth plates without specialist supervision
- Known hypersensitivity to hexarelin or formulation components
Frequently Asked Questions
Related Peptides
Experts Covering Hexarelin
LEGAL DISCLAIMER
The information provided on this page is for educational and informational purposes only and is not intended as medical advice. Hexarelin has not been approved by the FDA for any medical condition. Always consult with a qualified healthcare professional before starting any peptide therapy. Individual results may vary. Peptides Institute is not responsible for any adverse effects resulting from the use of information provided on this site.