货号 | 2976/50 |
别名 | 5-(4-Chlorophenyl)-N-(3,5-dimethoxy |
供应商 | Tocris |
生物活性 | 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. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 357.79 |
分子式 | C19H16ClNO4 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 25 mM in ethanol |
CAS号 | 944261-79-4 |
参考文献 | Kortet 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. McGaraughtyet 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. Jarviset 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. 1048520. 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. |