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5-(4-氯苯基)-N-(3,5-二甲氧基苯基)-2-呋喃甲酰胺

用途

A 803467是Nav1.8钠离子通道阻断剂,IC50为8 nM,比对Nav1.2,1.3,1.5和1.7的抑制性高100倍。

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名称

[ CAS 号 ]:
944261-79-4

[ 中文名 ]:
5-(4-氯苯基)-N-(3,5-二甲氧基苯基)-2-呋喃甲酰胺

[ 英文名 ]:
A-803467

[英文别名 ]:

cc-433
A-803467

生物活性

[ 描述 ]:

A 803467是Nav1.8钠离子通道阻断剂,IC50为8 nM,比对Nav1.2,1.3,1.5和1.7的抑制性高100倍。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

[参考文献]

[1]. McGaraughty, et al. 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. Journal of Pharmacology and Experimental Therapeutics (2008),

[2]. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5.

[3]. Joshi SK, et al. Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models. http://www.ncbi.nlm.nih.gov/pubmed/19070548

[4]. Kort ME, et al. Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
450.6±45.0 °C at 760 mmHg

[ 熔点 ]:
128-130?C

[ 分子式 ]:
C₁₉H₁₆ClNO₄

[ 分子量 ]:
357.788

[ 闪点 ]:
226.3±28.7 °C

[ 精确质量 ]:
357.076782

[ PSA ]:
60.70000

[ LogP ]:
4.93

[ 外观性状 ]:
white to tan

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.611

[ 储存条件 ]:
Store at +4°C

[ 水溶解性 ]:
DMSO: >10mg/mL

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2932190090

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海关

[ 海关编码 ]: 2932190090

[ 中文概述 ]:
2932190090 其他结构上有非稠合呋喃环化合物. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932190090 other compounds containing an unfused furan ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

文献

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Proc. Natl. Acad. Sci. U. S. A. 104 , 8520-5, (2007)

Activation of tetrodotoxin-resistant sodium channels contributes to action potential electrogenesis in neurons. Antisense oligonucleotide studies directed against Na(v)1.8 have shown that this channel...

Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels.

Mol. Interv. 7 , 192-5, (2007)

Voltage-gated sodium channels in nociceptive neurons are attractive targets for novel pain therapeutics. Although drugs that target voltage-gated sodium channels have proven value as pain therapeutics...

Functional Nav1.8 channels in intracardiac neurons: the link between SCN10A and cardiac electrophysiology.

Circ. Res. 111 , 333-43, (2012)

The SCN10A gene encodes the neuronal sodium channel isoform Na(V)1.8. Several recent genome-wide association studies have linked SCN10A to PR interval and QRS duration, strongly suggesting an as-yet u...

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