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Submit ReviewA 803467 is a selective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively). Shows no significant activity against TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.
A 803467 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 | 357.79 |
公式 | C19H16ClNO4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 944261-79-4 |
PubChem ID | 16038374 |
InChI Key | VHKBTPQDHDSBSP-UHFFFAOYSA-N |
Smiles | ClC(C=C2)=CC=C2C1=CC=C(C(NC3=CC(OC)=CC(OC)=C3)=O)O1 |
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 | 35.78 | 100 | |
ethanol | 8.94 | 25 |
以下数据基于产品分子量 357.79。 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 | 2.79 mL | 13.97 mL | 27.95 mL |
5 mM | 0.56 mL | 2.79 mL | 5.59 mL |
10 mM | 0.28 mL | 1.4 mL | 2.79 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Rush and Cummins (2007) Painful research: identification of a small-molecule inhibitor that selectively targets NaV1.8 sodium channels. Mol.Interv. 7 192 PMID: 17827438
McGaraughty et al (2008) A selective NaV1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J.Pharmacol.Exp.Ther. 324 1204 PMID: 18089840
Kort et al (2008) Discovery and biological evaluation of 5-Aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. J.Med.Chem. 51 407 PMID: 18176998
Jarvis et al (2007) A-803467, a potent and selective NaV1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc.Natl.Acad.Sci. 104 8520 PMID: 17483457
If you know of a relevant reference for A 803467, please let us know.
关键词: A 803467, A 803467 supplier, Selective, NaV18, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, A803467, Voltage-gated, 2976, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 803467 的部分引用包括:
Mascanfroni et al (2015) Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α. Biol Open 21 638 PMID: 26005855
Curtright et al (2015) Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery. PLoS One 10 e0116766 PMID: 25587718
Stone et al (2013) Attenuation of autonomic reflexes by A803467 may not be solely caused by blockade of NaV 1.8 channels. Nat Med 543 177 PMID: 23523647
Schuelert and McDougall (2012) Involvement of Nav 1.8 sodium ion channels in the transduction of mechanical pain in a rodent model of osteoarthritis. Arthritis Res Ther 14 R5 PMID: 22225591
Bladen (2012) Common mechanisms of drug interactions with sodium and T-type calcium channels. Mol Pharmacol 82 481 PMID: 22695716
Wu et al (2016) CXCL13/CXCR5 enhances sodium channel Nav1.8 current density via p38 MAP kinase in primary sensory neurons following inflammatory pain Scientific Reports 6 34836 PMID: 27708397
Liu et al (2014) Functional upregulation of nav1.8 sodium channels on the membrane of dorsal root Ganglia neurons contributes to the development of cancer-induced bone pain. PLoS One 9 e114623 PMID: 25503076
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