ProTx-III

ProTx-III, new selective Nav1.7 blocker

ProTx-III，新的選擇性Nav1.7通道阻斷劑

ProTx-III (µ-TRTX-Tp1a; belongs to NaSpTx family 1) has been isolated from the venom of the Peruvian green-velvet tarantula Thrixopelma pruriens at the University of Queensland (Australia). ProTx-III has been described to be a selective inhibitor of Na_v1.7 with an IC50 value around 2 nM. The synthetic version of Tp1a produced by Smartox yields similar results in terms of Na_v1.7 inhibition (see Figure 1). Queensland scientists have described that ProTx-III induces no significant changes in the voltage dependence of activation or steady-state inactivation of Na_v1.7. ProTx-III also inhibits Na_v1.1, Na_v1.2 and Na_v1.6 at nanomolar concentrations and does not affects Cav channels and nicotinic acetylcholine receptors. ProTx-III demonstrates analgesic propertiesin vivo when injected intraplantary in mice prior treatment with OD1, an activator of Na_v1.7, which induces spontaneous pain.

Fig 1: effect of 5nM Smartox ProTx-III on hNav1.7 current studied by eliciting voltage steps from -60 to +40 mV at a holding potential of -90 mV.

ProTx-III技術(shù)資料

氨基酸序列：

Asp-Cys²-Leu-Lys-Phe-Gly-Trp-Lys-Cys⁹-Asn-Pro-Arg-Asn-Asp-Lys-Cys¹⁶-Cys¹⁷-Ser-Gly-Leu-Lys-Cys²²-Gly-Ser-Asn-His-Asn-Trp-Cys²⁹-Lys-Leu-His-Ile-NH₂

二硫鍵：Cys²-Cys¹⁷, Cys⁹-Cys²², Cys¹⁶-Cys²⁹

長度 (aa)： 33

分子式： C₁₆₂H₂₄₆N₅₂O₄₃S₆

分子量：3802.47 Da

外觀：White lyophilized solid

可溶性： Water or saline buffer, 5 mg/mL maximum (recommendation)

Counterion: TFA salts

CAS 號：not available 

來源：Synthetic

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