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. 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. These GH-releasing peptides have no sequence similarity to ghrelin, but mimic ghrelin by acting as agonists at the ghrelin receptor, a G-protein-coupled receptor, designated GHS-R1a, expressed predominantly in the hypothalamic–pituitary region. In addition to neuroendocrine effects, hexarelin was reported to demonstrate non-endocrine pleiotropic effects in the cardiovascular system as well as in neoplastic tissues.

It has been reported previously that hexarelin binds to a novel class of binding sites in the mammalian heart that are distinct from the ghrelin receptor. The novel receptor was identified as CD36, a multifunctional type B scavenger receptor, expressed in various tissues, including monocytes/macrophages and the microvascular endothelium. In monocytes/macrophages, CD36 signalling leads to the activation of pro-inflammatory genes by the endothelium and to the scavenging of oxidized low-density lipoprotein, thereby predisposing to the atherogenic formation of foam cells, the first step in the development of fatty streak lesions. In agreement with this, it has been demonstrated that long-term administration of GHRPs to apoE (apolipoprotein E)-deficient mice fed a high-fat, high-cholesterol diet significantly reduced atherosclerotic lesion development in a CD36-dependent manner. The molecular basis of the binding of hexarelin to CD36 is of key importance for understanding the anti-atherosclerotic properties of this peptide.

Hexarelin substantially and dose-dependently increases plasma levels of growth hormone (GH) in animals and man. It releases more GH than does GHRH in humans, and produces synergistic effects on GH release in combination with GHRH, resulting in a major increases in plasma GH levels even with only low doses of hexarelin. Pre-administration of GH blunts the GH-releasing effect of hexarelin, while, in contrast, fully abolishing the effect of GHRH. Pre-treatment with IGF-1 has been also shown to blunt the GH-elevating effect of hexarelin. Testosterone, testosterone enanthate, and ethinylestradiol, though not oxandrolone, have been found to significantly potentiate the GH-releasing effects of hexarelin 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 hexarelin in humans.

A partial and reversible tolerance to the GH-releasing effects of hexarelin occurs in humans with long-term administration (50–75% decrease in efficacy over the course of weeks to months).

Hexarelin also, similarly to GHRP-2 and GHRP-6, slightly and dose-dependently stimulates the release of prolactin, adrenocorticotropic hormone (ACTH), and cortisol in humans. There are conflicting reports on the ability of hexarelin 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.  Hexarelin does not affect plasma levels of glucose, luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH) in humans.

Description:

Hexarelin is a hexapeptide, member of the GHRPs; peptide containing 6 amino acid residues.

H-His-D-2-Me-Trp-Ala-Trp-D-Phe-Lys-NH2

Synonyms:

Hexarelin,140703-51-1, L-Histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide

Physical Appearance:

Sterile Filtered White lyophilized (freeze-dried) powder.

Specificity:

Hexarelin substantially and dose-dependently increases plasma levels of growth hormone (GH) in animals and humans. Also, similarly to 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 Hexarelin 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.  Hexarelin does not affect plasma levels of glucose, luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH) in humans.

Purity:

>99.8% (HPLC analysed).

Solubility:

Add 1 ml of sterile diluent and let the lyophilized pellet dissolve completely.

Stability:

Store lyophilized peptide at -20 °C. Reconstituted peptide can be stored at 4 °C for a limited period of time. The lyophilized peptide remains stable until the expiry date when stored at -20 °C (48 Months).

Source:
Biosynthesis

Usage: 

The Product is prepared for LABORATORY RESEARCH USE ONLY!!!. The product may not be used for other purposes!!!