Hexrarelin

Hexarelin (Examorelin)

⚠️ For research use only; not a marketed drug; human injection is strictly prohibited; WADA S2-listed banned substance

The most potent GH-releasing agent in the GHRP family; features a unique CD36 target; cardiac protection is its signature research highlight

Basic Information

– CAS: 140703-51-1; Acetate CAS: 208251-52-9

– Aliases: Examorelin, EP-23905, MF-6003

– Type: Hexapeptide (6aa), D-2-MeTrp-modified, with superior resistance to enzymatic degradation compared to GHRP-6

– Sequence: His-D-2MeTrp-Ala-Trp-D-Phe-Lys-NH₂

– Molecular formula: \(\boldsymbol{C_{47}H_{58}N_{12}O_{6}}\)

– Molecular weight: 887.05 Da

– Appearance: White lyophilized powder

– Solubility: Easily soluble in BAC antibacterial water / AA sterile water

Contains tryptophan (Trp), which is light-sensitive; store away from light at all times

Mechanism of Action

1. GHS-R1a (ghrelin receptor) agonist: Stimulates the pituitary gland to release GH and inhibits somatostatin; exhibits the highest GH release intensity among the GHRP series, while also elevating cortisol and prolactin levels

2. Unique CD36 receptor binding (core differentiating selling point): Does not rely on the GH/IGF-1 pathway; acts directly on cardiac muscle and vascular endothelium. Research directions: cardiomyoprotection, anti-myocardial fibrosis, repair of ischemic damage, and vascular endothelial research

3. Exhibits strong synergistic effects when used in combination with GHRH analogs (CJC/Sermorelin/Tesamorelin), significantly amplifying GH pulses

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> Clinical History: Previously advanced to a Phase II study for heart failure; subsequent projects were terminated, and the drug was not approved for marketing

Pharmacokinetics (for Research Reference)

– Half-life: Approximately 30–40 minutes after subcutaneous administration; pulsatile release of GH

– Characteristics: Prone to receptor desensitization (tachyphylaxis); frequent dosing gradually reduces the GH response; dosing frequency must be controlled in animal studies

Reconstitution & Storage (Laboratory Procedures)

1. Solvent: BAC antimicrobial water / AA sterile water

2. Example: 2 mg lyophilized vial + 1 mL BAC water → 2 mg/mL

3. Powder: Store long-term at -20°C in a sealed container, protected from light

4. After reconstitution: Refrigerate at 2–8°C and use within 2–4 weeks; do not freeze-thaw repeatedly; store away from light

5. Procedure: Slowly add water along the wall of the vial; gently roll the vial; do not shake vigorously to prevent tryptophan oxidation

Compliance Notice

1. Research-grade Hexarelin is intended solely for in vitro cell and animal experiments; human use is prohibited