Hexarelin
Examorelin
Overview
Hexarelin is a synthetic hexapeptide and one of the most potent growth hormone releasing peptides (GHRPs) developed. It is a ghrelin receptor agonist that produces robust GH release and has demonstrated additional cardioprotective effects independent of GH secretion. Hexarelin has been studied in clinical trials for cardiac protection following myocardial infarction and for GH deficiency making it one of the few GHRPs with a meaningful clinical evidence base beyond animal studies. Its potency exceeds that of GHRP-6 and GHRP-2 but its tendency to cause rapid desensitization limits continuous use.
Mechanism of Action
Hexarelin acts as a potent agonist at the ghrelin receptor (GHSR-1a) stimulating GH release from pituitary somatotrophs through a mechanism complementary to GHRH. It also binds to the CD36 scavenger receptor in cardiac tissue — a GH-independent mechanism through which it exerts direct cardioprotective effects including reduced ischemia-reperfusion injury improved cardiac function after infarction and anti-fibrotic effects. In the pituitary Hexarelin stimulates GH release more potently than GHRP-6 or GHRP-2 on a molar basis. However receptor desensitization occurs more rapidly with Hexarelin than with other GHRPs making continuous daily use ineffective. Pulsatile or cycled administration protocols are required to maintain GH-stimulating efficacy over time.
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Dosage Information
Typical Dose
100-200 mcg per dose
Frequency
2-3 times daily maximum — must be cycled to avoid desensitization
Administration
Subcutaneous injection
Notes
Often stacked with CJC-1295 or Sermorelin for synergistic GH release. Due to rapid desensitization use protocols of 4-6 weeks on with 4 weeks off recommended.
Compound Data
Molecular Formula
C47H58N12O6
Molecular Weight
887.00 g/mol
IUPAC Name
(2S)-6-amino-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(2-methyl-1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
PubChem CID
6918297Potential Side Effects
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Quick Facts
- Administration
- Subcutaneous injection
- Typical Dose
- 100-200 mcg per dose
- Frequency
- 2-3 times daily maximum — must be cycled to avoid desensitization
- References
- 0 curated + 1 from PubMed
- Evidence Score
- 12.3 / 100