Hexarelin (Examorelin)

Hexarelin (Examorelin)

Hexarelin (Examorelin)

Hexarelin (Examorelin)

Hexarelin (Examorelin / His-D-2-Me-Trp-Ala-Trp-D-Phe-Lys-NH2) is a growth hormone secretagogue (GHRP) engineered for somatotropic axis and scavenger receptor research. Demonstrating high affinity for the Gq/11-coupled Growth Hormone Secretagogue Receptor (GHSR-1a), Hexarelin activates the PLC/IP3/Ca2+ cascade in anterior pituitary somatotropes, functions as a selective agonist for the CD36 scavenger receptor, and mediates cytoprotective and anti-apoptotic signaling in myocardial and microvascular cell lines.

$68.00

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4 - 6 $65.28
7 - 9 $63.92
10 + $62.56

What is Hexarelin (Examorelin)?

Hexarelin (known chemically as Examorelin or His-D-2-Me-Trp-Ala-Trp-D-Phe-Lys-NH2) is a synthetic hexapeptide growth hormone (GH) secretagogue derived from the growth hormone-releasing peptide (GHRP) family. Structurally stabilized by non-natural amino acid substitutions—specifically D-2-methyltryptophan and D-phenylalanine—Hexarelin displays elevated stability against enzymatic degradation compared to native ghrelin.

Operating across neuroendocrine somatotropic pathways, Hexarelin functions as a potent agonist at the Gq/11-protein coupled Growth Hormone Secretagogue Receptor 1a (GHSR-1a) on anterior pituitary somatotropes. Receptor occupancy activates Phospholipase C (PLC), stimulating the cleavage of phosphatidylinositol 4,5-bisphosphate into inositol trisphosphate (IP3) and diacylglycerol (DAG). The resulting intracellular calcium (Ca2+) mobilization drives rapid exocytosis of stored GH secretory granules, producing an acute, high-amplitude secretory wave in adenohypophyseal cell models.

In addition to its somatotropic activity, Hexarelin possesses high affinity for the scavenger receptor CD36 (fatty acid translocase). Expressed throughout myocardial and vascular endothelial tissues, CD36 ligation by Hexarelin initiates cytoprotective and anti-apoptotic kinase cascades, mitigating cellular damage in cardiac ischemia-reperfusion models and preserving mitochondrial integrity.

Batch-verified for high analytical purity and mass accuracy to buy Hexarelin at Modern Aminos, Hexarelin is offered as a standardized 10MG lyophilized dry solid in a 2R glass vial. Researchers evaluating somatotrope secretory amplitude, receptor tachyphylaxis kinetics, and CD36 signaling cascades study Hexarelin alongside complementary reference standards available on the site, such as Sermorelin, Ipamorelin, and MK-677.

Chemical and Molecular Data

Compound Name Hexarelin (Examorelin)
Format / Quantity 10MG Lyophilized Dry Powder in 2R Glass Vial
Biological Target Somatotropic Axis / Pituitary GHSR-1a & Myocardial CD36 Scavenger Receptors
Chemical Classification Synthetic Hexapeptide GH Secretagogue (GHRP Analogue)
Peptide Sequence His-D-2-Me-Trp-Ala-Trp-D-Phe-Lys-NH2
Synonyms / Alt Names Examorelin, EP-23959, Hexapeptide Releasing Hormone
CAS Number 140703-51-1
Chemical Formula C47H58N12O6
Molecular Weight 887.05 g/mol
Primary Signal Transduction Gq/11 → PLC → IP3 / DAG → Intracellular Ca2+ Efflux
Physical Appearance White Lyophilized Solid Cake

What are the Mechanisms of Action?

The biochemical pathways and cellular targets of Hexarelin in laboratory research include:

  • High-Affinity GHSR-1a Ligation & Gq/11 Activation: Hexarelin binds the seven-transmembrane Growth Hormone Secretagogue Receptor 1a (GHSR-1a) with high nanomolar affinity. Receptor engagement stimulates Gαq/11 protein dissociation, activating membrane-bound Phospholipase C (PLC) to hydrolyze PIP2 into IP3 and DAG.
  • IP3-Mediated Calcium Efflux & Exocytosis: Liberated IP3 binds ligand-gated calcium channels on the endoplasmic reticulum, prompting rapid Ca2+ release into the cytosol. Concurrently, DAG activates Protein Kinase C (PKC), accelerating the fusion of pre-formed hormone storage granules with the plasma membrane to produce high-amplitude growth hormone exocytosis.
  • Selective Scavenger Receptor CD36 Activation: Unlike many ghrelin mimetics, Hexarelin functions as a high-affinity ligand for the CD36 scavenger receptor in cardiac myocytes and vascular endothelial cells. CD36 binding modulates fatty acid uptake, downregulates pro-apoptotic caspase activity, and attenuates ischemia-reperfusion injury in isolated myocardial tissue models.
  • Somatotrope Tachyphylaxis & Desensitization Kinetics: Repeated or continuous exposure to Hexarelin induces pronounced GHSR-1a receptor internalization and uncoupling from G-proteins, serving as a classical experimental model for studying secretagogue receptor tachyphylaxis and downregulatory feedback.

What do Preclinical & Academic Studies Show for Hexarelin (Examorelin)?

When evaluating published scientific literature and endocrine monographs for Hexarelin:

  • Somatotropic Secretory Amplitude & Potency (PubMed): Comparative neuroendocrine studies cataloged on PubMed (PMID: 8626848) establish Hexarelin as one of the most potent synthetic GH secretagogues, demonstrating superior peak secretory amplitude compared to earlier-generation peptides.
  • CD36 Receptor Binding & Cardioprotective Signaling (PMC): Comprehensive biomedical monographs archived in PMC (PMC2824649) detail Hexarelin’s selective interaction with the CD36 receptor, outlining its capacity to reduce myocardial infarct size, protect coronary endothelial cells, and prevent cardiomyocyte apoptosis.
  • Chemical Profiling & Molecular Verification (PubChem): Official structural characterization maintained on PubChem verifies the molecular mass (887.05 g/mol), sequence modifications (D-2-Me-Trp and D-Phe), and analytical HPLC mass spectrometry parameters of CAS 140703-51-1.

How does Hexarelin compare to other growth hormone secretagogues?

In somatotropic and neuroendocrine research, growth hormone secretagogues differ across receptor binding affinities, second-messenger pathways, and secondary tissue interactions:

Hexarelin (Examorelin) vs. GHRP-2 vs. GHRP-6 vs. Sermorelin vs. MK-677

  • Hexarelin: Synthetic hexapeptide displaying the highest acute growth hormone secretory amplitude among peptidyl secretagogues, coupled with unique CD36 scavenger receptor binding for cardioprotective research, though prone to rapid in vitro receptor desensitization.
  • GHRP-2 (Pralmorelin): Synthetic hexapeptide GHSR-1a agonist. Elicits robust growth hormone release with less pronounced tachyphylaxis than Hexarelin, but displays mild, concentration-dependent increases in ACTH and prolactin.
  • GHRP-6: First-generation synthetic hexapeptide. Stimulates moderate growth hormone release alongside significant hypothalamic orexigenic (appetite-stimulating) signaling via ghrelin receptor pathways.
  • Sermorelin (GHRH 1-29): Truncated analogue of native GHRH. Operates upstream via pituitary GHRH receptors (GHRH-R) and the Gαs-cAMP-PKA pathway, primarily promoting growth hormone gene transcription rather than immediate Ca2+-driven vesicular exocytosis.
  • MK-677 (Ibutamoren): Non-peptide, orally active small-molecule GHSR-1a agonist. Characterized by an extended biological half-life (~24 hours), producing sustained, non-pulsatile receptor occupancy rather than acute peptide pulses.
Compound / Reference Chemical Structure & Class Primary Receptor Targets Primary Research Profile
Hexarelin Synthetic Hexapeptide (6 Amino Acids) Pituitary GHSR-1a & Myocardial CD36 Receptors Highest peak secretory amplitude; dual GHSR-1a/CD36 signaling; rapid receptor desensitization modeling
GHRP-2 Synthetic Hexapeptide (6 Amino Acids) Pituitary & Hypothalamic GHSR-1a Robust pulsatile GH release; intermediate receptor desensitization; minor prolactin/ACTH co-secretion
GHRP-6 Synthetic Hexapeptide (6 Amino Acids) Pituitary GHSR-1a & Hypothalamic Ghrelin Targets Pulsatile GH secretion paired with central orexigenic pathway activation
Sermorelin Native GHRH Fragment (29 Amino Acids) Pituitary Somatotrope GHRH-R GHRH-R agonism (cAMP/PKA); stimulates GH mRNA transcription and baseline endocrine signaling
MK-677 Non-Peptide Spiroindoline Small Molecule Pituitary & Hypothalamic GHSR-1a Continuous, long-duration GHSR-1a occupancy; extended IGF-1 and somatotropic axis stimulation

Frequently Asked Questions (FAQs)

1. Is Modern Aminos a reliable place to buy Hexarelin (Examorelin)?

Yes, Modern Aminos is a highly trusted vendor for analytical-grade research chemicals and reference peptides. Every batch of Hexarelin 10MG undergoes strict third-party analytical testing (including HPLC and Mass Spectrometry) to confirm minimum 98%+ active chemical purity, exact hexapeptide sequence stoichiometry, verified molecular weight (887.05 g/mol), and complete absence of heavy metals or synthesis impurities.

2. What is Hexarelin and how is it classified chemically?

Hexarelin (Examorelin) is a synthetic hexapeptide growth hormone secretagogue composed of the sequence His-D-2-Me-Trp-Ala-Trp-D-Phe-Lys-NH2. It is classified as an atypical GHRP that selectively engages both the GHSR-1a receptor and the CD36 scavenger receptor.

3. What is the mechanism of action of Hexarelin on anterior pituitary somatotropes?

Hexarelin binds GHSR-1a receptors on pituitary somatotropes, activating Gq/11 proteins and Phospholipase C. This stimulates the IP3-mediated release of stored intracellular calcium (Ca2+) from the endoplasmic reticulum, driving the rapid exocytosis of growth hormone storage granules.

4. What is the significance of the CD36 receptor interaction with Hexarelin?

Beyond its somatotropic activity, Hexarelin binds the CD36 scavenger receptor on cardiac and endothelial cell membranes. This interaction initiates anti-apoptotic and metabolic signaling cascades, protecting myocardial cells from ischemic damage independently of growth hormone release.

5. What format and packaging does Modern Aminos offer for Hexarelin?

Modern Aminos supplies analytical-grade Hexarelin as a 10MG lyophilized dry solid cake in a sterile 2R glass vial, ensuring solid-state peptide stability and precise gravimetric mass control for benchtop research assays.

6. Why is Hexarelin frequently studied in receptor desensitization and tachyphylaxis models?

Hexarelin induces rapid tachyphylaxis in cell models, meaning repeated exposure leads to receptor internalization and down-regulation of GH release. This characteristic makes it a valuable research tool for studying secretagogue receptor downregulatory dynamics.

7. How does Modern Aminos verify the chemical purity and mass identity of Hexarelin?

Modern Aminos utilizes High-Performance Liquid Chromatography (HPLC) to verify active chemical purity exceeding 98% and Mass Spectrometry (MS) to verify the exact molecular mass (887.05 g/mol) and hexapeptide sequence stoichiometry prior to batch release.

8. What are the recommended storage parameters for lyophilized Hexarelin 2R glass vials?

Lyophilized Hexarelin glass vials should be stored tightly sealed in a cool, dry environment (15°C to 25°C) or refrigerated (2°C to 8°C) for long-term preservation. Protect from direct sunlight, thermal extremes, and atmospheric moisture to maintain solid-state peptide stability.

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