OtherEvidence B2 cited

Argireline

aka Acetyl hexapeptide-3 · Acetyl hexapeptide-8 · Ac-EEMQRR-NH2

A topical hexapeptide that modulates the SNAP-25 protein complex to reduce expression lines. Functions as a topical alternative to botulinum toxin with a milder, non-paralytic mechanism.

Molecular wt
889.0g/mol
Formula
C34H60N14O12S
CAS
616204-22-9
Route
Topical / subcutaneous

Sequence

One-letter6 residues

Ac-EEMQRR-NH2

Three-letter

Ac-Glu-Glu-Met-Gln-Arg-Arg-NH2

Read this before quoting the sequence
N-terminally acetylated, C-terminally amidated hexapeptide (INCI names acetyl hexapeptide-3 and acetyl hexapeptide-8 refer to the same molecule). The sequence Ac-EEMQRR-NH2 is stated verbatim in the original 2002 paper. It mimics the N-terminal end of SNAP-25.
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Mechanism of action

Argireline inhibits the formation of the SNARE complex by competing with SNAP-25 for incorporation into the synaptic vesicle fusion machinery at the neuromuscular junction. This reduces neurotransmitter (acetylcholine) release, decreasing muscle contraction intensity without full paralysis. The result is a reduction in dynamic expression lines, particularly around the eyes and forehead. Unlike botulinum toxin, the effect is partial and reversible.

What the evidence actually shows

Grade B

Clinical studies demonstrate 10-30% reduction in wrinkle depth with 10% argireline solution applied twice daily for 30 days. Less potent than botulinum toxin but non-invasive. Consumer studies show visible improvement.

Regulatory status

Status
Cosmetic ingredient; not an approved drug. Regulated as a cosmetic ingredient (INCI acetyl hexapeptide-3 / acetyl hexapeptide-8) rather than as a medicine.
Clinical stage
Cosmetic efficacy studies only; no drug development programme identified.
WADA
USADA states that topical use of a growth factor or peptide is as prohibited as injectable or oral forms, but also notes that GlobalDRO lists certain cosmetic peptides (including hexapeptide variants) as non-prohibited. Argireline was not named in any official source retrieved, so no definitive status is asserted here.
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Dosing — what backs each figure

Argireline (acetyl hexapeptide-8) is a topical cosmetic ingredient, not an injectable. Asking for its 'dose' in mg/day is a category error: published human studies specify a formulation concentration applied to the skin twice daily for about 4 weeks, and the Cosmetic Ingredient Review panel has only assessed it as safe up to 0.005% in cosmetic products. There is no injectable or systemic dose for argireline in any published source, and its poor penetration of the stratum corneum means it is not expected to reach neuromuscular junctions in the first place.

ClinicalApproved labelling or a published human trial
PreclinicalAnimal studies — not a human dose
  • Applied to the skin twice daily for 6 weeks in D-galactose-induced aged mice; improved skin histology and type I collagen. Concentration not stated in abstract.

    mouse · topical · PMID 23464592

Animal doses do not convert to human doses by body weight alone. Route matters too — a compound dosed intraperitoneally in mice tells you little about subcutaneous use.

No established human dose
No approved label or completed human trial establishes a dosing regimen for this compound. Anything presented as a standard protocol for it — anywhere — is someone's convention rather than a finding.

Handling and storage

Lyophilized
No compound-specific data documented
Reconstituted
No compound-specific data documented
Solvent
Water (the original efficacy study used a 10% aqueous hexapeptide phase in an oil/water emulsion)

No stability/storage study for argireline as a raw material was located in a primary or regulatory source. It contains a methionine residue (verified from the formula/structure), which is chemically oxidation-prone, but no measured stability figures were found. No compound-specific stability study (lyophilised or reconstituted) was located in a primary/regulatory source during this verification pass. Only generic synthetic-peptide handling guidance exists for this compound; no specific temperatures or durations are recorded here rather than fabricating them.

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Safety

References (2)

Data provenance

Chemistry and citations on this page were checked against primary sources on 2026-08-14. Values that could not be verified were left blank rather than filled with a plausible guess.

Could not verify
storage.lyophilized, storage.reconstituted, storage.lightSensitive

Research use only
This profile is educational reference material. It is not medical advice, not a prescription, and not an endorsement of self-administration. Compounds discussed here are research chemicals and most are not approved for human therapeutic use.