GHRP-2 Technical Specification Sheet

Molecular Properties

Parameter Value
Chemical Name Growth Hormone Releasing Peptide-2 / Pralmorelin
Amino Acid Sequence D-Ala-D-2-Nal-Ala-Trp-D-Phe-Lys-NH₂
Molecular Formula C₄₅H₅₅N₉O₆
Molecular Weight 817.97 g/mol
CAS Number 158861-67-7
Sequence Length 6 amino acids (synthetic hexapeptide with D-amino acids)
Receptor Target Growth Hormone Secretagogue Receptor 1a (GHS-R1a) / Ghrelin receptor

Physical Properties

Property Specification
Appearance White to off-white lyophilized powder
Solubility Soluble in water or bacteriostatic water at ≥1 mg/mL; pH 5.5-7.5
pH (1% solution) 5.5 - 7.5
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]⁺ = 817.97 ± 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/Ghrelin Research 200-600 μg/kg 30-60 min before measurements SC or IP
Note: Dosing information is for research reference only. GHRP-2 is intended for laboratory research. Mimics ghrelin action at GHS-R1a receptor; stimulates appetite and GH release.

Key Research Studies

Year Study Focus Key Findings
1995 Discovery and characterization of GHS-R GHRP-2 identified as potent synthetic ligand for orphan GPCR (later named GHS-R1a); demonstrated EC₅₀ of 0.1-1 nM for GH release; 10-100x more potent than GHRH in vitro
1999 Synergy with GHRH Combined GHRP-2 + GHRH administration produced synergistic GH response (5-10x vs either alone); demonstrated distinct receptor mechanisms and complementary signaling pathways
2006 Appetite stimulation and orexigenic effects GHRP-2 (300 μg/kg SC) increased food intake by 40-60% within 2 hours; activated NPY/AgRP neurons in arcuate nucleus; effects blocked by GHS-R1a antagonists
2012 Cardioprotective and anti-inflammatory effects GHRP-2 treatment (200 μg/kg twice daily) reduced infarct size by 30-40% in cardiac ischemia models; decreased inflammatory markers (IL-6, TNF-α); GHS-R1a-dependent and independent mechanisms identified

Mechanism of Action

Biological Pathway Description
GHS-R1a Activation Binds ghrelin receptor (GHS-R1a), Gq-coupled GPCR; high affinity (Kd ~0.5-5 nM); expressed in pituitary, hypothalamus, heart, adipose
GH Secretion Activates pituitary somatotrophs → PLC/PKC pathway → Ca²⁺ mobilization → GH release; peak GH at 15-30 minutes post-dose
Hypothalamic Effects Stimulates arcuate NPY/AgRP neurons → appetite increase; modulates GHRH neuron activity; amplifies endogenous GH pulses
Peripheral Actions Cardioprotection via GHS-R1a-dependent and independent mechanisms; anti-inflammatory effects; modulation of adipocyte function
Half-Life 20-30 minutes (IV/SC); D-amino acids provide resistance to peptidases vs natural peptides

Comparative Analysis: GHRP Family

Compound MW (Da) GH Potency Appetite Effect Cortisol/Prolactin
GHRP-2 817.97 High (EC₅₀ ~0.1-1 nM) Strong (+40-60%) Moderate increase
GHRP-6 872.44 High (EC₅₀ ~0.2-2 nM) Very strong (+60-100%) Moderate increase
Hexarelin 887.04 Very high (EC₅₀ ~0.05-0.5 nM) Moderate (+20-40%) Strong increase
Ipamorelin 711.85 Moderate (EC₅₀ ~1-10 nM) Minimal No increase (selective)

Quality Control Parameters

Test Method Acceptance Criteria
Appearance (visual) White to off-white powder; no aggregation
Chiral Purity D-amino acids at positions 1, 2, 5 confirmed; >98% correct stereochemistry
RP-HPLC (purity) Main peak ≥98.0%; no single impurity >0.5%
ESI-MS (identity) [M+H]⁺ = 817.97 ± 0.5 Da confirmed
Biological Activity ≥85% potency vs reference in GH release assay

Structure-Activity Relationship

Position Amino Acid Structural Role
1 D-Ala N-terminal stability; prevents aminopeptidase degradation
2 D-2-Nal (D-2-naphthylalanine) Critical for receptor binding; aromatic interaction with GHS-R1a
3 L-Ala Conformational spacer
4 L-Trp Essential for activity; indole ring interactions
5 D-Phe Receptor selectivity; D-configuration critical
6 L-Lys-NH₂ C-terminal; positive charge; amidation essential

Reported Biological Effects

Effect Category Observed Changes Timeframe
GH Secretion Peak GH increase 5-20x baseline; occurs 15-30 min post-dose; duration 1-2 hours Acute (minutes to hours)
IGF-1 Levels Increased 30-50% with repeated dosing; cumulative effect over 1-2 weeks 7-14 days
Appetite Increased food intake 40-60%; peak effect 1-3 hours post-dose Acute (1-4 hours)
Body Composition Increased lean mass 2-5%; modest fat reduction with chronic dosing 4-8 weeks

External References

1. Bowers CY, et al. On the in vitro and in vivo activity of a new synthetic hexapeptide that acts on the pituitary to specifically release growth hormone. Endocrinology. 1984;114(5):1537-45. https://pubmed.ncbi.nlm.nih.gov/6143887/

2. Smith RG, et al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev. 1997;18(5):621-45. https://academic.oup.com/edrv/article/18/5/621/2548680

3. National Center for Biotechnology Information. PubChem Compound Summary for GHRP-2. https://pubchem.ncbi.nlm.nih.gov/compound/GHRP-2

Disclaimer: This product is intended for research use only. Not for human or veterinary diagnostic or therapeutic use. GHRP-2 is a potent GHS-R1a agonist with both GH-releasing and orexigenic properties.