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Submit ReviewPF 05089771
说明： Potent and selective Nav1.7 channel blocker
化学名： 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
纯度： ≥98% (HPLC)
生物活性 for PF 05089771
PF 05089771 is a potent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for PF 05089771
PF 05089771 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PF 05089771
| 分子量 | 672.56 |
| 公式 | C18H12Cl2FN5O3S2.C7H8O3S |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1430806-04-4 |
| PubChem ID | 71554187 |
| InChI Key | NVKBPDYKPNYMDR-UHFFFAOYSA-N |
| Smiles | ClC1=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C(F)C(S(NC4=CSC=N4)(=O)=O)=C1.CC5=CC=C(S(=O)(O)=O)C=C5 |
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 PF 05089771
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 67.26 | 100 |
制备储备液 for PF 05089771
以下数据基于产品分子量 672.56。 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 | 1.49 mL | 7.43 mL | 14.87 mL |
| 5 mM | 0.3 mL | 1.49 mL | 2.97 mL |
| 10 mM | 0.15 mL | 0.74 mL | 1.49 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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产品说明书 for PF 05089771
参考文献 for PF 05089771
参考文献是支持产品生物活性的出版物。
Cao et al (2016) Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci.Transl.Med. 8 335ra56 PMID: 27099175
Alexandrou et al (2016) Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release. PLoS One 11 e0152405 PMID: 27050761
Swain et al (2017) Discovery of clinical candidate 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): design and optimization of diaryl ether aryl sulfonamides as selective inhibitors of Na J.Med.Chem. 60 7029 PMID: 28682065
If you know of a relevant reference for PF 05089771, please let us know.
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关键词: PF 05089771, PF 05089771 supplier, PF05089771, potent, selective, Nav1.7, sodium, channels, neuropathic, pain, Voltage-gated, Sodium, Channels, 5931, Tocris Bioscience
6 篇 PF 05089771 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 05089771 的部分引用包括：
Jing et al (2021) A central mechanism of analgesia in mice and humans lacking the sodium channel NaV1.7. Neuron 109 1497-1512.e6 PMID: 33823138
Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762
Ellen A et al (2019) Tetrodotoxin-Sensitive Sodium Channels Mediate Action Potential Firing and Excitability in Menthol-Sensitive Vglut3-Lineage Sensory Neurons. J Neurosci 39 7086-7101 PMID: 31300524
Oliver et al (2023) Bringing to light the physiological and pathological firing patterns of human induced pluripotent stem cell-derived neurons using optical recordings. Front Cell Neurosci 16 1039957 PMID: 36733665
Wei et al (2023) Ectopic expression of Nav1.7 in spinal dorsal horn neurons induced by NGF contributes to neuropathic pain in a mouse spinal cord injury model. Front Mol Neurosci 16 1091096 PMID: 36937049
Darik A et al (2022) NaV1.1 is essential for proprioceptive signaling and motor behaviors. Elife 11 PMID: 36278870
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PF 05089771 的评论
平均评分: 5 (Based on 1 Review.)
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Study of PF 05089771's Nav1.7 blocking efficacy.
By
Anonymous on 12/26/2019
种属： Human
The effect of PF-05089771, a selective, peripherally restricted Nav1.7 sodium channel blocker on pain due to diabetic peripheral neuropathy was investigated.
