GHRP-6 Technical Specification Sheet

Molecular Properties

Parameter Value
Chemical Name Growth Hormone Releasing Peptide-6
Amino Acid Sequence His-D-Trp-Ala-Trp-D-Phe-Lys-NH₂
Molecular Formula C₄₆H₅₆N₁₂O₆
Molecular Weight 872.44 g/mol
CAS Number 87616-84-0
Sequence Length 6 amino acids (synthetic hexapeptide with D-amino acids)
Receptor Target Growth Hormone Secretagogue Receptor 1a (GHS-R1a) / Ghrelin receptor; CD36 (additional effects)

Physical Properties

Property Specification
Appearance White to off-white lyophilized powder
Solubility Soluble in water or bacteriostatic water at ≥1 mg/mL; pH 5.0-7.0
pH (1% solution) 5.0 - 7.0
Hygroscopicity Low to moderate; standard desiccated storage
Solution Stability Stable at 4°C for 10-14 days; D-amino acids enhance stability

Analytical Specifications

Test Specification
HPLC Purity ≥98.0%
Mass Spectrometry Confirmed [M+H]⁺ = 872.44 ± 0.5 Da
Peptide Content ≥95% (by amino acid analysis)
Endotoxin Level <1.0 EU/mg
Acetate Content ≤5%
TFA Content ≤0.1%
Water Content ≤6% (Karl Fischer)

Storage Parameters

Condition Specification
Lyophilized Storage -20°C, desiccated
Lyophilized Shelf Life 24-36 months when stored properly
Reconstituted Storage 2-8°C for up to 14 days; -20°C for up to 3 months
Reconstitution Protocol Add 1-2 mL sterile water or bacteriostatic water to 5 mg vial; gentle vortex 30 seconds
Freeze-Thaw Cycles Tolerates up to 5 cycles; D-amino acids provide stability
Light Sensitivity Low; standard laboratory storage acceptable

Research Dosing Reference

Application Typical Dose Range Frequency Route
In Vitro Pituitary Cell Assays 10-1000 nM Acute stimulation (30 min to 2 hours) Culture media
Small Animal Models (Rodent) 50-500 μg/kg 1-3x daily SC or IV
GH Secretion Studies 100-300 μg/kg Single dose or BID/TID for 7-28 days SC preferred
Appetite/Feeding Studies 200-800 μg/kg 30-60 min before feeding measurements SC or IP
Note: Dosing information is for research reference only. GHRP-6 is intended for laboratory research. Notable for strongest appetite-stimulating effects among GHRPs.

Key Research Studies

Year Study Focus Key Findings
1984 Initial discovery and GH-releasing activity First synthetic hexapeptide GHRP identified by Bowers group; demonstrated potent GH release with EC₅₀ of 0.2-2 nM in vitro; 100-1000x more potent than GHRH on molar basis
1996 Appetite stimulation and food intake GHRP-6 (300-600 μg/kg SC) increased food intake by 60-100% within 2 hours; effect mediated via hypothalamic NPY/AgRP neurons; strongest orexigenic effect among early GHRPs
2002 CD36 receptor interaction Identified CD36 (fatty acid translocase) as secondary target for GHRP-6; mediated anti-inflammatory and cardioprotective effects independent of GHS-R1a; Ki ~100-500 nM at CD36
2008 Dual receptor mechanism characterization GHRP-6 effects dissected: GH release via GHS-R1a (blocked by [D-Lys3]-GHRP-6); appetite via GHS-R1a; wound healing and fibrosis effects via CD36; demonstrated unique dual-target pharmacology

Mechanism of Action

Biological Pathway Description
GHS-R1a Activation (Primary) Binds ghrelin receptor (GHS-R1a), Gq-coupled GPCR; high affinity (Kd ~0.5-5 nM); stimulates GH release and appetite
GH Secretion Activates pituitary somatotrophs → PLC/PKC → Ca²⁺ mobilization → GH release; peak GH at 20-40 minutes post-dose; pulsatile pattern
Appetite Stimulation Activates arcuate NPY/AgRP neurons; strongest hunger effect in GHRP family; increases ghrelin-like orexigenic signaling; food intake peaks 1-3 hours post-dose
CD36 Receptor Effects Binds CD36 (moderate affinity); anti-inflammatory actions; modulates fatty acid uptake; cardioprotective and wound healing properties
Half-Life 20-30 minutes (IV/SC); D-amino acids provide peptidase resistance

Comparative Analysis: GHRP-6 vs GHRP-2

Parameter GHRP-6 GHRP-2
Sequence Position 1 L-His D-Ala
Sequence Position 2 D-Trp D-2-Nal
GH Release Potency High (EC₅₀ ~0.2-2 nM) High (EC₅₀ ~0.1-1 nM)
Appetite Stimulation Very strong (+60-100%) Strong (+40-60%)
CD36 Interaction Yes (moderate affinity) Minimal
Clinical Development Research tool Advanced to human trials

Quality Control Parameters

Test Method Acceptance Criteria
Appearance (visual) White to off-white powder; no aggregation or discoloration
Chiral Purity D-amino acids at positions 2 and 5 confirmed; >98% correct stereochemistry
RP-HPLC (purity) Main peak ≥98.0%; no single impurity >0.5%
ESI-MS (identity) [M+H]⁺ = 872.44 ± 0.5 Da confirmed
Biological Activity ≥85% potency vs reference in GH release assay

Structure-Activity Relationship

Position Amino Acid Structural Role
1 L-His N-terminal; imidazole ring; pH-dependent charge; distinguishes from GHRP-2
2 D-Trp Critical for receptor binding; D-configuration essential for activity and stability
3 L-Ala Conformational spacer; small side chain
4 L-Trp Essential for GHS-R1a activation; indole ring interactions
5 D-Phe Receptor selectivity; D-configuration prevents degradation
6 L-Lys-NH₂ C-terminal; positive charge; amidation absolutely required

Reported Biological Effects

Effect Category Observed Changes Timeframe
GH Secretion Peak GH increase 5-15x baseline; occurs 20-40 min post-dose; duration 1-2 hours Acute (minutes to hours)
IGF-1 Elevation Increased 30-60% with repeated dosing; cumulative with chronic administration 7-14 days
Appetite/Food Intake Increased food intake 60-100%; strongest effect in GHRP class; peak 1-3 hours Acute (1-4 hours)
Anti-inflammatory Reduced inflammatory markers; CD36-mediated effects; cardio/wound healing benefits 24-72 hours

External References

1. Bowers CY, et al. Structure-activity relationships of a synthetic pentapeptide that specifically releases growth hormone in vitro. Endocrinology. 1981;108(3):1070-6. https://pubmed.ncbi.nlm.nih.gov/6109621/

2. Demers A, et al. Growth hormone-releasing peptides: a potential multifaceted treatment for the heart. Recent Pat Cardiovasc Drug Discov. 2011;6(1):52-9. https://pubmed.ncbi.nlm.nih.gov/21208158/

3. National Center for Biotechnology Information. PubChem Compound Summary for GHRP-6. https://pubchem.ncbi.nlm.nih.gov/compound/GHRP-6

Disclaimer: This product is intended for research use only. Not for human or veterinary diagnostic or therapeutic use. GHRP-6 exhibits the strongest appetite-stimulating effects in the GHRP family.