GsMtx-4

Inhibitory Cystine Knot (ICK) Peptide / Mechanosensitive Channel BlockerRx: ResearchCompound: Research

Also known as: Grammostola spatulata mechanotoxin 4, GsMTx4, Piezo channel inhibitor peptide

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

GsMtx-4 is a 34-amino acid peptide toxin originally isolated from the venom of the tarantula Grammostola spatulata (now Grammostola rosea). It is the first selective inhibitor of mechanosensitive ion channels and has been extensively used as a research tool to study the role of Piezo1, Piezo2, and other SACs in mechanotransduction. Potential therapeutic applications include atrial fibrillation, muscular dystrophy, neuropathic pain, and pulmonary hypertension, but it remains a research compound with no approved clinical use.

Mechanism of Action

Selectively inhibits mechanosensitive ion channels, particularly Piezo1, Piezo2, and certain stretch-activated cation channels (SACs), by partitioning into the lipid bilayer and altering membrane tension-dependent gating rather than directly blocking the channel pore; acts as a gating modifier toxin.

Routes of Administration

IntrathecalIntravenousSubcutaneousTopical (research)

Goals & Uses

  • Muscular dystrophy (Duchenne) treatmentNeuromuscular DiseaseLow
  • Research tool – mechanotransduction studiesResearchHigh
  • Atrial fibrillation suppressionCardiovascularLow
  • Neuropathic pain reliefPain / NeurologyLow
  • Pulmonary arterial hypertensionCardiovascular / PulmonaryLow

Contraindications

  • Known hypersensitivity to spider venom peptidesAllergy / ImmunologyHigh
  • Human clinical useRegulatoryHigh

Adverse Effects

  • Cardiovascular depressionCardiovascularUnknown
  • Immune/allergic reactionImmunologicalUnknown
  • Off-target channel inhibitionPharmacologicalUncommon

Drug Interactions

  • Other mechanosensitive channel modulatorsLow

Population Constraints

  • Pregnant or lactating individualsReproductiveRelative
  • Pediatric populationsAgeRelative
  • Patients with cardiac arrhythmiasCardiovascularRelative

Regulatory Status

  • European UnionUnapprovedNo EMA approval or investigational status; research reagent only.
  • United StatesUnapprovedResearch use only; not an IND-filed compound as of available data. Available commercially from peptide suppliers for laboratory use.
  • United KingdomUnapprovedNo MHRA approval; research reagent only.

Not approved by any regulatory agency (FDA, EMA, MHRA) for clinical use. Available as a synthetic research peptide for laboratory and preclinical studies only.

Evidence & Sources

No sources recorded yet.

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