GX 201

Pricing Availability   Qty
说明: Potent and selective Nav1.7 blocker; analgesic
化学名: 4-[[1-[[2-Chloro-5-(trifluoromethyl)phenyl]methyl]-4-piperidinyl]methoxy]-5-cyclopropyl-2-fluoro-N-(methylsulfonyl)benzamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for GX 201

GX 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.

化合物库 for GX 201

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。

技术数据 for GX 201

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.

溶解性数据 for GX 201

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 56.3 100

制备储备液 for GX 201

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for GX 201

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


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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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