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Submit ReviewProTx II is a selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.
分子量 | 3826.59 |
公式 | C168H250N46O41S8 |
序列 |
YCQKWMWTCDSERKCCEGMVCRLWCKKKLW (Modifications: Disulfide bridges: 2-16, 9-21, 15-25) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 484598-36-9 |
PubChem ID | 118708662 |
InChI Key | XOAUGYVLRSCGBG-ZJDFQAAZSA-N |
Smiles | [H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O)[C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N3)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC2=O)C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性 | Soluble to 1 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Smith et al (2007) Molecular interactions of the gating modifier toxin ProTx-II with NaV 1.5: implied existence of a novel toxin binding site coupled to activation. J.Biol.Chem. 282 12687 PMID: 17339321
Edgerton et al (2008) Evidence for multiple effects of ProTxII on activation gating in NaV 1.5. Toxicon. 52 489 PMID: 18657562
Schmalhofer et al (2008) ProTx-II, a selective inhibitor of NaV 1.7 sodium channels, blocks action potential propagation in nociceptors. Mol.Pharmacol. 74 1476 PMID: 18728100
Xu et al (2019) Structural basis of Nav1.7 inhibition by a gating-modifier spider toxin. Cell. 176 702 PMID: 30661758
If you know of a relevant reference for ProTx II, please let us know.
关键词: ProTx II, ProTx II supplier, toxins, voltage, gated, sodium, Na+, channels, NaV1.7, potent, selective, blockers, venoms, Voltage-gated, Sodium, Channels, 4023, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ProTx II 的部分引用包括:
Shen et al (2019) Structures of human Nav1.7 channel in complex with auxiliary subunits and animal toxins. Science 363 1303 PMID: 30765606
Li et al (2017) Membrane protein Nav1.7 contributes to the persistent post-surgical pain regulated by p-p65 in dorsal root ganglion (DRG) of SMIR rats model. BMC Anesthesiol 17 150 PMID: 29115943
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