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Submit ReviewGX 201 is a potent and selective Nav1.7 blocker (IC50 = 3.2 nM). Exhibits 10x selectivity for Nav1.7 over Nav1.1, Nav1.2, and Nav1.6 channels. Displays prolonged residency time on the Nav1.7 channel. Chronic dosing increases compound potency ~10-fold and provides efficacy that persists after the compound has cleared from plasma. Suppresses neuropathic pain in a mouse diabetic neuropathy model. Analgesic.
GX 201 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 563 |
公式 | C25H27ClF4N2O4S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1788071-27-1 |
PubChem ID | 118120545 |
InChI Key | KYBPOTYVFWNSGS-UHFFFAOYSA-N |
Smiles | CS(=O)(NC(C1=CC(C2CC2)=C(C=C1F)OCC3CCN(CC3)CC4=CC(C(F)(F)F)=CC=C4Cl)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 56.3 | 100 |
以下数据基于产品分子量 563。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.78 mL | 8.88 mL | 17.76 mL |
5 mM | 0.36 mL | 1.78 mL | 3.55 mL |
10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
参考文献是支持产品生物活性的出版物。
Shields et al (2018) Insensitivity to pain upon adult-onset deletion of NaV1.7 or its blockade with selective inhibitors J.Neurosci. 38 10180 PMID: 30301756
Banker et al (2018) Selective NaV1.7 antagonists with long residence time show improved efficacy against inflammatory and neuropathic pain. Cell Rep. 24 3133 PMID: 30231997
If you know of a relevant reference for GX 201, please let us know.
关键词: GX 201, GX 201 supplier, GX201, Potent, selective, Nav1.7, voltage-gated, Sodium, NaV, Channels, blockers, blocks, inhibitors, inhibits, neuropathic, pain, slow, dissociation, Voltage-gated, 7029, Tocris Bioscience
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