ProTx II;
ProTx II 是 Nav1.7 钠通道的选择性阻滞剂,IC50 值为 0.3 nM,对 Nav1. 7的选择性是其他钠通道亚型的至少 100 倍。ProTx-II 通过降低通道电导和将激活的电压转移到更多的正电位来抑制钠离子通道,并阻止伤害感受器中动作电位的传播。
ProTx II Chemical Structure
CAS No. : 484598-36-9
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是否有货 |
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100 mg |
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250 mg |
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500 mg |
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* Please select Quantity before adding items.
生物活性 |
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors[1][2].
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IC50 Target |
IC50: 0.3 nM (NaV1.7), 41 nM (Nav1.2), 102 nM (NaV1.3), 39 nM (NaV1.4), 79 nM (NaV1.5), 26 nM (NaV1.6), 146 nM (NaV1.8)[1]
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Formula |
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Sequence Shortening |
YCQKWMWTCDSERKCCEGMVCRLWCKKKLW (Disulfide bridge:Cys2-Cys16;Cys9-Cys21;Cys15-Cys25)
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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[1]. Tanaka K, et al. Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. J Exp Pharmacol. 2015 Jun 24;7:11-6.
[2]. Schmalhofer WA, et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol. 2008 Nov;74(5):1476-84.
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