Hexarelin Acetate/Cas No.: 140703-51-1
Purity (HPLC): 98.0%
Appearance: White powder
Molecular Formula: C47H58N12O6
Molecular Weight: 887.04
Single Impurity (HPLC): 0.5%max
Amino Acid Composition: ±10% of theoretical
Peptide Content (N%): ≥80.0%
Water Content(Karl Fischer): ≤8.0%
Acetate Content(HPIC): ≤10.0%
Specific Rotation (20/D): -55.0～-65.0°(c=1 1%HAc)
Mass Balance: 95.0~105.0%
treatment of growth hormone deficiency
congestive heart failure
Examorelin (INN) (developmental code names EP-23905, MF-6003), also known as hexarelin, is a potent, synthetic, peptidic, orally-active, centrally-penetrant, and highly selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and a growth hormone secretagogue which was developed by Mediolanum Farmaceutici.It is a hexapeptide with the amino acid sequence His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 which was derived from GHRP-6 (which, in turn, is an analogue of ghrelin).
Examorelin substantially and dose-dependently increases plasma levels of growth hormone (GH) in animals and humans. In addition, similarly to pralmorelin (GHRP-2) and GHRP-6, it slightly and dose-dependently stimulates the release of prolactin, adrenocorticotropic hormone (ACTH), and cortisol in humans.There are conflicting reports on the ability of examorelin to elevate insulin-like growth factor 1 (IGF-1) and insulin-like growth factor-binding protein 1 (IGFBP-1) levels in humans, with some studies finding no increase and others finding a slight yet statistically significant increase.Examorelin does not affect plasma levels of glucose, luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH) in humans.
Examorelin releases more GH than does growth hormone-releasing hormone (GHRH) in humans,and produces synergistic effects on GH release in combination with GHRH, resulting in "massive" increases in plasma GH levels even with only low doses of examorelin.Pre-administration of GH blunts the GH-releasing effect of examorelin, while, in contrast, fully abolishing the effect of GHRH. Pre-treatment with IGF-1 also blunts the GH-elevating effect of examorelin. Testosterone, testosterone enanthate, and ethinyl estradiol, though not oxandrolone, have been found to significantly potentiate the GH-releasing effects of examorelin in humans. In accordance, likely due to increases in sex steroid levels, puberty has also been found to significantly augment the GH-elevating actions of examorelin in humans.
A partial and reversible tolerance to the GH-releasing effects of examorelin occurs in humans with long-term administration (50-75% decrease in efficacy over the course of weeks to months).
Examorelin reached phase II clinical trials for the treatment of growth hormone deficiency and congestive heart failure.