COGNITIVEPreclinicalMEMORYCOGNITIVE ENHANCEMENTALZHEIMER'S

Dihexa

Also known as: PNB-0408 · N-hexanoic-Tyr-Ile-(6)-aminohexanoic amide

12.5k views/week 89 citations 0 edits Updated 5/24/2026

Dihexa is a potent peptidomimetic derived from angiotensin IV that acts as a superagonist of the HGF/MET signaling system. It has demonstrated cognitive-enhancing effects up to 7 orders of magnitude more potent than BDNF in rodent models of Alzheimer's disease, making it one of the most powerful pro-cognitive compounds under investigation.

STRUCTURE

Molecular Composition

FORMULA
C₂₅H₄₁N₃O₄
MOL. WEIGHT
451.62 Da
CAS NUMBER
1401708-83-5
TARGET
HGF / MET receptor
DERIVED FROM
Angiotensin IV
BBB PENETRANT
Yes (oral/transdermal)
AMINO ACID CHAIN VISUALIZATION
N
N-Hexanoyl cap
lipophilic cap, BBB penetration
NH-CO
Y
Tyrosine
HGF-MET pharmacophore, core contact
NH-CO
I
Isoleucine
hydrophobic spacer, conformation
NH-CO
A
ε-aminohexanoic amide
biostable tail, MET potentiation
SEQUENCEN-Y-I-A
MECHANISMS

How It Works

HGF/MET Receptor Superagonism
Dihexa potentiates hepatocyte growth factor (HGF) binding to the MET receptor tyrosine kinase in neurons — functioning as an HGF superagonist with EC50 in the femtomolar range. MET activation triggers PI3K/Akt/mTOR (synapse formation), ERK1/2 (neuroplasticity gene transcription), and MAPK/CREB (long-term memory consolidation) cascades simultaneously.
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Synaptogenesis — ~10M× More Potent Than BDNF
In hippocampal neuron cultures, Dihexa induces dendritic spine formation and new synapse growth with an EC50 approximately 7 orders of magnitude lower than BDNF for this specific endpoint (Bhaskaran et al., 2013). Hippocampal slices show increased synaptophysin and PSD-95 expression — structural markers of new synapse formation — and enhanced long-term potentiation (LTP) amplitude.
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Blood-Brain Barrier Penetration
Unlike BDNF, HGF, and NGF themselves — which fail to cross the BBB — Dihexa's small size (451 Da) and lipophilicity enable CNS penetration after oral or transdermal administration. Brain/plasma ratios in rodents support effective hippocampal delivery. This BBB permeability is the key pharmacological advantage enabling its cognitive-enhancing effects via peripheral dosing.
Reversal of Age-Related Cognitive Decline
In aged rats with established spatial memory deficits (18-month Morris Water Maze impairment), 5 days of Dihexa treatment restored performance to young-animal levels — effects persisting beyond the drug elimination period. Scopolamine-induced amnesia was fully reversed at 1 mg/kg SC. The durable post-treatment benefit suggests neuroplasticity-based mechanisms rather than acute pharmacology.
OVERVIEW

Research Overview

Dihexa was developed at Washington State University by Joseph Harding and Joseph Wright, published in 2013. It is a small, orally bioavailable peptidomimetic built on the angiotensin IV (Ang IV) scaffold, modified to resist peptidase degradation and enhance CNS penetration. Its primary mechanism — potentiation of HGF/MET signaling — is distinct from all other nootropic peptides.

In animal models of Alzheimer's dementia, Dihexa reversed cognitive impairment at doses 10 million times lower than BDNF, the gold standard benchmark. It promotes synaptogenesis (new synapse formation) rather than merely protecting existing synapses, making it theoretically capable of structural cognitive restoration rather than just preservation.

Mechanism of Action

// HGF/MET SUPERAGONISM

Dihexa potentiates the binding of Hepatocyte Growth Factor (HGF) to its receptor c-MET, a receptor tyrosine kinase expressed broadly in neurons. HGF/MET signaling drives synaptogenesis, dendritic arborization, and neuronal survival — processes that are deficient in Alzheimer's disease and cognitive aging.

// SYNAPSE FORMATION

By amplifying HGF/MET downstream signaling (PI3K/Akt and MAPK/ERK), Dihexa significantly increases synaptic density in the hippocampus and prefrontal cortex — areas critical for memory formation and executive function. This structural remodeling is detectable by electron microscopy in treated animals.

DOSAGE

Dosage & Administration

TRANSDERMAL
DOSE
1–10 mg in DMSO/ethanol vehicle
FREQUENCY
Once daily
NOTES
Preferred route in rodent studies — skin application in DMSO vehicle achieved brain concentrations sufficient for cognitive enhancement. Apply to thin-skinned areas (inner wrist, inner arm). DMSO vehicle must be pharmaceutical grade. Transdermal delivery provides slower, more sustained CNS levels compared to SC injection. Research context only.
INJECTABLE (SUBCUTANEOUS)
DOSE
1–5 mg
FREQUENCY
Once daily or every other day
NOTES
Used in key rodent cognitive studies (1 mg/kg SC achieved full reversal of scopolamine-induced cognitive impairment and restoration of aged-rat spatial memory). Reconstitute in DMSO/PEG-400 co-solvent mixture due to limited aqueous solubility. Research context only — no human clinical trials published.

Dihexa is one of the most potent synthetic nootropics in preclinical research — ~10 million-fold more potent than BDNF for synaptogenesis in hippocampal neurons (in vitro assay). Its effects appear to persist beyond drug elimination, suggesting structural synaptic remodelling rather than purely pharmacological mechanisms. Long-term human safety is not characterised. No human clinical trials published as of 2025.

CYCLING

Cycle Duration Guide

ON CYCLE
4–8 weeks
OFF CYCLE
4 weeks off minimum

Given that Dihexa's cognitive effects appear to persist post-washout (structural synaptic remodelling), cycle protocols include mandatory off periods to assess baseline cognition and avoid potential cumulative effects. The HGF/MET pathway promotes neuroplasticity — chronic overstimulation of growth factor receptors warrants caution. No established human protocol; rodent studies used 5-day to 4-week treatment windows.

No published human clinical trial data. Long-term safety profile unknown. HGF/MET receptor signalling promotes cell growth — theoretical concern for individuals with pre-existing malignancies. Not recommended without thorough medical evaluation. Research context only.

Quick Reference
FORMULAC₂₄H₄₀N₄O₄
MOL. WEIGHT448.6 Da
LENGTH2 amino acids
ORIGINSynthetic peptidomimetic derived from the angiotensin IV scaffold; developed at Washington State University
HALF-LIFEOrally bioavailable; estimated half-life 12–24 hours. Good CNS penetration.
SOLUBILITYSoluble in DMSO; limited water solubility — often formulated in propylene glycol or ethanol
CAS NO.1401708-83-5
STATUSPreclinical
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TAGS
memorycognitive enhancementAlzheimer'sHGFMET receptorsynaptogenesis