ProTx-III
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia.
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- CAS. Nr.: 1808297-63-3
- Formel: C162H246N52O43S6
- Molecular Weight:3802.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Nav1.7 2.1 nM (IC50) |
ProTx-III in native, recombinant and synthetic C-terminal acid and amide forms inhibit hNaV1.7 with IC50s of 2.1, 9.5, 11.5 and 2.5 nM, respectively[1].
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ProTx-III inhibits hNav1.7 without significantly altering the voltage dependence of activation or inactivation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OD1-induced mouse model of pain(300Nm; intraplantar injection)[1]
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Dosage:100 nM, 300 nM, 1μM
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Administration:intraplantar injection
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Result:Showed at 1 μM (40 pmoles in a 40 μl injection) and 300 nM (12 pmoles in a 40 μl injection) significantly reduced spontaneous pain behaviour in a concentration dependent manner and this reduction in pain behaviour persisted for 25 min after injection of the highest concentration.
Chemical Information
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CAS. Nr. 1808297-63-3
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Molecular Weight 3802.40
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Formel C162H246N52O43S6
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Synonyms
μ-TRTX-Tp1a
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Sequence
Asp-Cys-Leu-Lys-Phe-Gly-Trp-Lys-Cys-Asn-Pro-Arg-Asn-Asp-Lys-Cys-Cys-Ser-Gly-Leu-Lys-Cys-Gly-Ser-Asn-His-Asn-Trp-Cys-Lys-Leu-His-Ile-NH2 (Disulfide bonds: Cys2-Cys17, Cys9-Cys22, Cys16-Cys29)
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Sequence Shortening
DCLKFGWKCNPRNDKCCSGLKCGSNHNWCKLHI-NH2 (Disulfide bonds: Cys2-Cys17, Cys9-Cys22, Cys16-Cys29)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)