BPC-157
Technical Monograph
BPC-157 (Body Protective Compound-157) is a synthetic pentadecapeptide derived from a protein isolated from human gastric juice. It is investigated in preclinical models for its observed cytoprotective properties across multiple tissue types.
Mechanism of Action
BPC-157 activates multiple signaling cascades. Primary pathways include: (1) FAK-paxillin pathway activation - increases migratory potential of tendon fibroblasts and promotes cell adhesion; (2) VEGFR2-Akt-eNOS pathway - time-dependent activation of VEGFR2 leading to pro-angiogenic effects and eNOS-derived NO production; (3) ERK1/2 pathway activation with downstream targets c-Fos and c-Jun; (4) JAK-2 pathway activation specifically through increased phosphorylation levels as downstream signal of growth hormone receptor; (5) Modulation of FoxO3a, p-AKT, p-mTOR, and p-GSK-3β expression; (6) Upregulation of antioxidant proteins including heme oxygenase (HO-1) and NQO-1.
Pharmacological Detail
Interacts with the BP3 receptor and activates intracellular signaling cascades including the FAK-paxillin pathway and PI3K/Akt pathway, influencing cell survival and migration in vitro.
Pharmacodynamics
Parenteral applications rapidly replenish depleted intracellular reserves. It demonstrates highly synergistic reductions in mass markers and stimulates tissue remodeling pathways.
Pharmacokinetics
Highly localized activity. In humans, plasma concentrations returned to baseline within 24 hours following IV infusion with a half-life of <30 minutes. Bioavailability reaches 14-19% (IM in rats) and 45-51% (IM in dogs). Tmax is observed at 3.00 minutes (rats) to 8.67 minutes (dogs).
Preclinical Observations & In Vitro Data
Extensive preclinical data supports its role in experimental models of tissue repair. Early human pilot data indicates high tolerability for intra-articular and systemic routes.
Pharmacokinetic Profile
- Receptor Affinity: High affinity for BP3 receptor
- Terminal Half-Life: < 30 minutes (Human IV); ~15 mins (Rats IV)
- Peak Systemic Saturation (Tmax): 3.00 minutes (Rats IM), 6.33-8.67 mins (Dogs IM)
- Molecular Stability: High gastric stability; susceptible to UV degradation.
Observed Timeline of Action
| Timeframe | Pharmacological Effect |
|---|---|
| 2 Hours | Injury severity score reduced. Lesions attenuated with less hematoma/edema. |
| Day 1 | Improved motor function. Increased desmin positivity. Inflammatory phase initiated. |
| Day 3 | Growth hormone receptor expression peaks at 7-fold increase in tendon fibroblasts. |
| Day 14 | Repair/proliferative phase peak. Achilles tendon shows full integrity reestablished. |
| Day 90 | MRI shows 0mm gap in muscle-detachment models. Well-organized cortical bone and mature fibers. |
| 6-12 Months | Clinical: Sustained knee pain relief reported in human retrospective pilots. |
Abstract Highlights
- Actin-sequestering properties documented in vitro
- Upregulation of actin and cellular motility markers
- Observed angiogenic signaling modulation
- Counteraction of pro-inflammatory cytokines (IL-6, TNF-alpha)
References
Chemical Specifications
Material Handling & Stability
Strict Notice
THIS COMPOUND IS PRODUCED FOR LABORATORY RESEARCH PURPOSES ONLY. NOT FOR HUMAN CONSUMPTION. MATERIAL DATA SHEETS AND LABORATORY GUIDELINES SHOULD BE CONSULTED PRIOR TO HANDLING.