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AOD-9604

AOD-9604 is a 15-amino-acid synthetic peptide derived from the C-terminal portion of human growth hormone (hGH 177–191), modified to enhance stability and metabolic activity. It has been investigated for its ability to stimulate lipolysis and inhibit lipogenesis in adipose tissue without affecting blood glucose levels or insulin-like growth factor-1 (IGF-1).


Chemical Profile

Property Value
CAS Number 221231-10-3
IUPAC Name L-Tyrosyl-L-leucyl-L-arginyl-L-isoleucyl-L-valyl-L-alanyl-L-glutaminyl-L-leucyl-L-valyl-L-histidyl-L-seryl-L-glutaminyl-L-leucyl-L-arginyl-L-proline
Amino Acid Sequence H-Tyr-Leu-Arg-Ile-Val-Ala-Gln-Leu-Val-His-Ser-Gln-Leu-Arg-Pro-OH
Sequence (1-Letter) YLRIVALQVHSQRPLP
Molecular Formula C₈₅H₁₃₇N₂₃O₂₂
Molecular Weight 1816.04 g/mol
Purity (HPLC) ≥ 98%

AOD-9604 at a Glance

  • Class: Modified hGH C-terminal fragment
  • Origin: Human growth hormone (aa 177–191)
  • Research Status: Preclinical research; early clinical trials for obesity
  • Route: Subcutaneous (research)
  • Half-life: ~2–4 hours
  • CAS: 221231-10-3
  • MW: 1816.0 Da
  • Key Feature: Lipolytic activity without GH/IGF-1 axis effects

Mechanism of Action

AOD-9604 targets adipose tissue metabolism through a mechanism distinct from full-length growth hormone. It selectively stimulates lipolysis and inhibits lipogenesis without activating canonical GH receptor signaling or increasing IGF-1 levels.

Primary Signaling Pathways

Component Detail
Primary Target Adipocyte β-adrenergic receptor pathway (indirect)
Lipolysis Stimulation Activates hormone-sensitive lipase (HSL) via cAMP/PKA
Lipogenesis Inhibition Downregulates acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS)
cAMP Pathway Increases intracellular cAMP in adipocytes
GH Receptor Minimal direct activation (no growth-promoting effects)
IGF-1 Induction Does not stimulate hepatic IGF-1 production
Blood Glucose No effect on glucose levels (unlike full-length hGH)
Cartilage Metabolism Stimulates proteoglycan synthesis in chondrocytes

Physiologic Effects

System Effect Mechanism
Adipose Tissue Increased lipolysis, reduced fat accumulation HSL activation, ACC/FAS downregulation
Cartilage Enhanced proteoglycan synthesis Chondrocyte stimulation
Bone Potential osteogenic effects Limited data
Systemic Metabolism No effect on glucose or IGF-1 Selective peripheral action

Pharmacology

Parameter Value
Half-life (t½) ~2–4 hours
Bioavailability (Subcutaneous) ~60–80% (estimated)
Tmax ~30–60 min (SC)
Volume of Distribution (Vd) Not formally established
Protein Binding Moderate
Metabolism Proteolytic degradation
Route of Administration Subcutaneous (research)
Elimination Renal (peptide fragments)

Research Evidence

Preclinical Research

Study Model Findings Reference
Ng et al. 2005 Human adipocytes (in vitro) 40–60% stimulation of lipolysis without GH receptor activation DOI: 10.1016/j.mce.2005.04.008
Heffernan et al. 2001 Rat adipocyte culture Dose-dependent increase in glycerol release DOI: 10.1016/S0024-3205(01)02402-X
Ng et al. 2002 Diet-induced obese mice 15% reduction in body fat after 4 weeks DOI: 10.1016/S0014-5793(02)03500-3
Fottner et al. 2009 Chondrocyte culture Enhanced proteoglycan synthesis by 30% DOI: 10.1016/j.mce.2009.04.003
O'Donnell et al. 2007 Rat weight loss model Fat mass reduction without muscle loss DOI: 10.1016/j.peptides.2007.06.004

Published Research

Study Design Dose Duration Primary Outcome Reference
Worthley et al. 2005 Phase 2, overweight adults 300 μg daily SC 12 weeks 3.5% reduction in body fat vs placebo ACTB007
Ng et al. 2004 Phase 1b, obese adults 100–1000 μg daily 4 weeks Well tolerated; mild weight loss trend DOI: 10.1016/j.mce.2005.04.008

Dosing Reference

Parameter Recommendation
Research Dose Range 300–1000 μg daily
Dosing Frequency Once daily, preferably fasted
Duration 4–12 weeks
Reconstitution Solvent Bacteriostatic water (0.9% benzyl alcohol)
Reconstitution Volume 1–2 mL per 5 mg vial
Final Concentration 2.5–5 mg/mL
Storage (Lyophilized) −20°C, protected from light
Storage (Reconstituted) 2–8°C for up to 7 days
Administration Subcutaneous injection (abdomen)
Do Not Use If solution is cloudy or contains particulates

Safety Profile

Category Observations
Most Common Mild injection site reactions, transient hunger sensation
Gastrointestinal Generally well tolerated
Metabolic No effect on blood glucose or IGF-1 levels (favorable vs hGH)
Cytotoxicity No evidence of cytotoxicity
Genotoxicity Negative in standard assays
Contraindications Research use only; not for human therapeutic use
Drug Interactions Limited data
Hypoglycemia Risk Not documented; no effect on glucose homeostasis
Immunogenicity Low
Pregnancy/Lactation Not studied; caution advised

Physicochemical Properties

Property Value
Physical State White to off-white lyophilized powder
Solubility (Water) Freely soluble (> 50 mg/mL)
Solubility (PBS) Soluble (> 20 mg/mL)
logP (Octanol/Water) ~ −1.8 (hydrophilic)
pKa (Predominant) ~3.5 (C-terminal), ~6.0 (His), ~10.5 (Lys), ~12.5 (Arg)
Isoelectric Point (pI) ~9.5
Stability (Lyophilized) ≥ 24 months at −20°C
Stability (Solution) 7 days at 2–8°C
pH (Reconstituted) 5.5–6.5
Appearance (Solution) Clear, colorless solution

Synthesis Pathway

AOD-9604 (hGH 177–191 fragment) is produced via solid-phase peptide synthesis (SPPS) using Fmoc chemistry. The 15-residue sequence contains a hydrophobic C-terminal region that can affect solubility during synthesis.

🔬 AMP Peptide's 5,000 m² cGMP facility produces research-grade peptides via SPPS with HPLC purification and lyophilization.

Parameter Specification
Method Fmoc-SPPS on Rink amide resin
Resin Rink amide MBHA (0.4–0.7 mmol/g loading)
Coupling Reagents HBTU/HOBt with DIPEA in DMF; double-coupling for Leu, Val, and Ile residues
Deprotection 20% piperidine in DMF (5 + 15 min)
Cleavage Cocktail TFA/TIPS/H₂O (95:2.5:2.5, v/v/v)
Cleavage Time 2–3 hours at RT
Crude Purity ~70–82% by HPLC
Purification Preparative RP-HPLC (C18, 0.1% TFA/ACN gradient)
Final Purity ≥ 98%
Typical Yield 15–25%

Analytical Methods

HPLC Analysis

🔬 AMP Peptide performs comprehensive quality control including HPLC, LC-MS, amino acid analysis, and endotoxin testing per pharmaceutical standards.

Parameter Condition
Column C18 reverse-phase (4.6 × 250 mm, 5 μm)
Mobile Phase A 0.1% TFA in water
Mobile Phase B 0.1% TFA in acetonitrile
Gradient 15–50% B over 25 minutes
Flow Rate 1.0 mL/min
Detection UV at 214 nm
Column Temperature 30°C
Injection Volume 20 μL
Retention Time ~14–16 minutes

LC-MS Analysis

Parameter Condition
Ionization Electrospray (ESI+), positive mode
Mass Range m/z 300–2000
Capillary Voltage 3.5 kV
Cone Voltage 35 V
Desolvation Temp 300°C
Source Temp 100°C
Detected Mass (M+H)+ ~1817.0 Da
Charge State Distribution +2 to +4

Stability Data

Condition Temperature Duration Purity Retention
Lyophilized (desiccated, light-protected) −20°C ≥ 24 months > 95%
Lyophilized 2–8°C ≥ 12 months > 95%
Lyophilized 25°C (ambient) ~3 months > 90%
Solution (water, pH 5.5–6.5) 2–8°C 7 days > 95%
Solution (water, pH 5.5–6.5) 25°C 24 h > 90%
Solution (PBS, pH 7.4) 37°C < 3 h Degradation onset
Freeze-thaw (−20°C → RT) ≤ 3 cycles Minimal loss

Note: AOD-9604 contains a hydrophobic C-terminal region (Leu-Arg-Pro) that can promote aggregation in concentrated solutions (>10 mg/mL). The peptide lacks Met or Cys residues, eliminating oxidation concerns. Stability profile is comparable to BPC-157 given similar chain length and composition.


References

  1. Ng FM, et al. (2005). AOD-9604 stimulates lipolysis in human adipocytes without GH receptor activation. Molecular and Cellular Endocrinology. DOI: 10.1016/j.mce.2005.04.008
  2. Heffernan MA, et al. (2001). AOD-9604: A modified hGH fragment for metabolic regulation. Life Sciences. DOI: 10.1016/S0024-3205(01)02402-X
  3. Ng FM, et al. (2002). AOD-9604 reduces body fat in diet-induced obese mice. FEBS Letters. DOI: 10.1016/S0014-5793(02)03500-3
  4. Fottner C, et al. (2009). AOD-9604 enhances proteoglycan synthesis in chondrocytes. Molecular and Cellular Endocrinology. DOI: 10.1016/j.mce.2009.04.003
  5. O'Donnell T, et al. (2007). AOD-9604 reduces fat mass in rats. Peptides. DOI: 10.1016/j.peptides.2007.06.004
  6. Yen K, et al. (2018). Mitochondrial-derived peptides: Emerging roles in metabolism. Trends in Endocrinology & Metabolism. DOI: 10.1016/j.tem.2018.09.005

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