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PTX003-ProTx-III,新的選擇性Nav1.7通道阻斷劑
【產(chǎn)品簡(jiǎn)介】
【詳細(xì)說(shuō)明】
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 Nav1.7 with an IC50 value around 2 nM. The synthetic version of Tp1a produced by Smartox yields similar results in terms of Nav1.7 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 Nav1.7. ProTx-III also inhibits Nav1.1, Nav1.2 and Nav1.6 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 Nav1.7, 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(zhǎng)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(hào):not available
來(lái)源:Synthetic
產(chǎn)品信息
貨號(hào) | 名稱 | 規(guī)格 |
PTX003 | ProTx-III | 100ug/500ug/1000ug/5×10ug |
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