5-(4-氯苯基)-N-(3,5-二甲氧基苯基)-2-呋喃甲酰胺

更新时间：2025-08-22 00:55:34

5-(4-氯苯基)-N-(3,5-二甲氧基苯基)-2-呋喃甲酰胺结构式	常用名	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
	CAS号	944261-79-4	分子量	357.788
	密度	1.3±0.1 g/cm3	沸点	450.6±45.0 °C at 760 mmHg
	分子式	C₁₉H₁₆ClNO₄	熔点	128-130?C
	MSDS	中文版美版	闪点	226.3±28.7 °C
	符号	GHS07	信号词	Warning

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。

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	5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
英文别名	更多

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.

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.

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
InChIKey	VHKBTPQDHDSBSP-UHFFFAOYSA-N
SMILES	COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1
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

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

5-(4-chlorophen...

57753-80-7

3,5-二甲氧基苯胺

10272-07-8

5-(4-氯苯基)-N-(3,...

944261-79-4

文献：Journal of Medicinal Chemistry, , vol. 51, # 3 p. 407 - 416

上游产品 2
CAS号57753-80-7 5-(4-chlorophen... CAS号10272-07-8 3,5-二甲氧基苯胺
下游产品 0

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%

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...

5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furamide

cc-433

A-803467