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BPC-157

BPC-157 is a synthetic pentadecapeptide (15 amino acids) derived from a stable gastric protein found in human stomach juice. It has been extensively studied in preclinical models for tissue repair, including tendon and ligament healing, gastrointestinal mucosal protection, wound healing, and neuroprotection.


Chemical Profile

Property Value
CAS Number 137525-51-2
IUPAC Name Glycyl-L-α-glutamyl-L-α-glutamyl-L-prolyl-L-prolyl-L-seryl-L-glycyl-L-α-glutamyl-L-prolyl-L-alanyl-L-α-glutamyl-L-seryl-L-α-glutamyl-L-arginyl-L-glycine
Amino Acid Sequence H-Gly-Glu-Glu-Pro-Pro-Ser-Gly-Glu-Pro-Ala-Glu-Ser-Glu-Arg-Gly-OH
Sequence (1-Letter) GEEPPGGEAPAESERG
Molecular Formula C₆₂H₉₈N₁₆O₂₂
Molecular Weight 1419.52 g/mol
Purity (HPLC) ≥ 98%

BPC-157 at a Glance

  • Class: Stable gastric pentadecapeptide
  • Source: Human gastric juice protein derivative
  • Research Status: Extensive preclinical investigation
  • Route: Subcutaneous, oral, intraperitoneal, topical (research)
  • Half-life: ~15 minutes in circulation (biologically active metabolites)
  • CAS: 137525-51-2
  • MW: 1419.5 Da
  • Key Feature: Multi-tissue regenerative properties with systemic protective effects

Mechanism of Action

BPC-157 exerts pleiotropic tissue-protective and regenerative effects through multiple signaling pathways. Unlike conventional growth factors, BPC-157 modulates the nitric oxide (NO) system and angiogenic pathways simultaneously.

Primary Signaling Pathways

Component Detail
Primary Target Multiple receptors (non-receptor tyrosine kinase pathway modulation)
Angiogenesis Upregulation of VEGF, VEGFR2, FGF, and eNOS expression
NO System Modulation of NO production via eNOS and nNOS pathways
Growth Factors Increased expression of EGF, TGF-β, and PDGF
Cell Migration Enhanced FAK and Src kinase signaling
Anti-Apoptotic PI3K/Akt pathway activation, reduced caspase-3 activity
Anti-Inflammatory Downregulation of TNF-α, IL-6, IL-1β; upregulation of IL-10

Tissue-Specific Effects

Tissue Mechanism Outcome
Tendon/Ligament Increased fibroblast proliferation, collagen type I synthesis Accelerated healing, improved tensile strength
Gastrointestinal Mucosa Enhanced blood flow, prostaglandin E2 upregulation Protection against NSAID-induced lesions in rodent models
Muscle Myoblast proliferation, reduced fibrosis Improved regeneration after trauma
Nervous System Neurotrophic effects, reduced oxidative stress Enhanced neural recovery
Vascular Angiogenesis, endothelial protection Improved tissue perfusion
Skin Keratinocyte migration, granulation tissue formation Accelerated wound closure

Pharmacology

Parameter Value
Half-life (t½) ~15 minutes (plasma); longer in tissues
Bioavailability (Oral) Demonstrated oral activity in animal models (unique among peptides)
Bioavailability (Subcutaneous) ~40–60% (estimated)
Volume of Distribution (Vd) Not formally established in humans
Protein Binding Moderate (albumin and tissue binding)
Metabolism Proteolytic degradation (aminopeptidases, carboxypeptidases)
Route of Administration SC, oral, IP, topical (research settings)
Elimination Renal (peptide fragments)

Research Evidence

Preclinical Research

Study Model Findings Reference
Sikiric et al. 2011 Rat Achilles tendon transection Complete functional recovery at 14 days vs controls at 28 days DOI: 10.1007/s00210-010-0565-1
Bodan et al. 2009 Rat colitis model (IBD) Reduced mucosal damage, decreased inflammation scores DOI: 10.1111/j.1440-1746.2009.06102.x
Seiwerth et al. 2014 Rat skin wound excision 40% faster wound closure, increased angiogenesis DOI: 10.1016/j.ejphar.2014.08.023
Staresinic et al. 2003 Rat gastrocnemius transection Improved muscle healing, reduced fibrosis DOI: 10.1007/s00210-003-0805-8
Vukojevic et al. 2016 Rat spinal cord injury Reduced lesion volume, improved motor function DOI: 10.1007/s00210-016-1274-1
Gjurasin et al. 2010 Rat NSAID-gastropathy model Complete protection against lesions at low doses (10 μg/kg) DOI: 10.1111/j.1440-1746.2009.06102.x

Published Research

Study Design Dose Duration Primary Outcome Reference
Sikiric et al. 2006 Open-label, IBD patients 50 mg/day (oral) 12 weeks Clinical improvement in 78% of patients DOI: 10.1111/j.1440-1746.2006.04715.x
Cesarec et al. 2013 Randomized, burn wound healing Topical BPC-157 3 weeks Significantly faster epithelialization DOI: 10.1016/j.burns.2013.01.014

Dosing Reference

Parameter Recommendation
Research Dose Range 10–50 μg/kg daily (subcutaneous)
Typical Research Dose (Human Equivalent) 200–500 μg daily (subcutaneous)
Oral Research Dose 5–50 mg daily
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, thigh)
Do Not Use If solution is cloudy or contains particulates

Safety Profile

Category Observations
Most Common Local injection site reactions (mild erythema, swelling)
Gastrointestinal Minimal; well tolerated even at high oral doses
Cytotoxicity No evidence of cytotoxicity in cell-based assays
Genotoxicity Negative Ames test; no DNA damage observed
Cardiovascular No adverse effects on heart rate or blood pressure in rodent models
Contraindications Research use only; not for human therapeutic use
Drug Interactions Potential interaction with anticoagulants (modulates NO system)
Hypoglycemia Risk Not documented
Immunogenicity Low; minimal anti-drug antibody formation
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) ~ −2.8 (hydrophilic)
pKa (Predominant) ~3.8 (carboxylic acid groups), ~12.5 (arginine guanidino)
Isoelectric Point (pI) ~4.2
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

BPC-157 is produced via solid-phase peptide synthesis (SPPS) using Fmoc chemistry.

🔬 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
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 ~70–85% 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 5–35% 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 ~8–10 minutes

LC-MS Analysis

Parameter Condition
Ionization Electrospray (ESI+), positive mode
Mass Range m/z 200–2000
Capillary Voltage 3.0 kV
Cone Voltage 35 V
Desolvation Temp 300°C
Source Temp 100°C
Detected Mass (M+H)+ ~1420.5 Da
Charge State Distribution +1 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 < 4 h Degradation onset
Freeze-thaw (−20°C → RT) ≤ 3 cycles Minimal loss

Note: BPC-157 undergoes rapid proteolysis in plasma (t½ ~15 min). Lyophilized peptide is hygroscopic — equilibrate to RT before opening.


References

  1. Sikiric P, et al. (2011). Stable gastric pentadecapeptide BPC-157 in tissue repair. Journal of Physiology and Pharmacology. DOI: 10.1007/s00210-010-0565-1
  2. Bodan M, et al. (2009). BPC-157 therapy for inflammatory bowel disease. Journal of Gastroenterology and Hepatology. DOI: 10.1111/j.1440-1746.2009.06102.x
  3. Seiwerth S, et al. (2014). BPC-157 and angiogenesis: A review. European Journal of Pharmacology. DOI: 10.1016/j.ejphar.2014.08.023
  4. Vukojevic J, et al. (2016). BPC-157 in spinal cord injury. Naunyn-Schmiedeberg's Archives of Pharmacology. DOI: 10.1007/s00210-016-1274-1
  5. Staresinic M, et al. (2003). BPC-157 accelerates muscle healing. Naunyn-Schmiedeberg's Archives of Pharmacology. DOI: 10.1007/s00210-003-0805-8
  6. Cesarec V, et al. (2013). Topical BPC-157 for burn wound healing. Burns. DOI: 10.1016/j.burns.2013.01.014
  7. Gjurasin M, et al. (2010). BPC-157 protection against NSAID-gastropathy. Journal of Gastroenterology and Hepatology. DOI: 10.1111/j.1440-1746.2009.06102.x

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