A3109
A-803467
≥98% (HPLC), Nav1.8 sodium channel blocker, powder
别名:
5-(4-氯苯基)-N-(3,5-二甲氧基苯基)呋喃-2-甲酰胺
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关于此项目
经验公式（希尔记法）:
C19H16NO4Cl
化学文摘社编号:
分子量:
357.79
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
A-803467, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to tan
溶解性
DMSO: >10 mg/mL
创始人
Abbott
储存温度
room temp
SMILES字符串
COc1cc(NC(=O)c2ccc(o2)-c3ccc(Cl)cc3)cc(OC)c1
InChI
1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22)
InChI key
VHKBTPQDHDSBSP-UHFFFAOYSA-N
相关类别
一般描述
A-803467能够抑制感觉神经元的自发和诱发动作电位。它具有镇痛作用。A-803467能够在体内减少脊髓背角神经元的放电。
小分子A-803467是一种有效的选择性Nav1.8钠离子通道阻滞剂。Nav1.8是一种抗河豚毒素（TTX-R）钠离子通道，通过在周围感觉神经元中传递疼痛刺激而产生痛觉；A-803467通过阻滞该通道，能够对多种模型产生不同程度的疼痛减轻作用。 A-803467已被用于进一步探究Nav1.8在传递疼痛刺激中的作用，也可用作镇痛药。
生化/生理作用
A-803467能够在半数最大无活性和静止状态下阻断Nav1.8，IC50分别为 8 nM和79 nM。A-803467对Nav1.8的选择性比人类Nav1.2、1.3、1.5和1.7高100倍。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Mihai Moldovan et al.
Neurobiology of aging, 39, 128-139 (2016-03-01)
Accumulating myelin abnormalities and conduction slowing occur in peripheral nerves during aging. In mice deficient of myelin protein P0, severe peripheral nervous system myelin damage is associated with ectopic expression of Nav1.8 voltage-gated Na(+) channels on motor axons aggravating the
Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad (2010)
Anthony M Rush et al.
Molecular interventions, 7(4), 192-195 (2007-09-11)
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, the drugs that are currently available are non-specific sodium channel inhibitors, which limit their
K Bekő et al.
Journal of thrombosis and haemostasis : JTH, 15(6), 1223-1235 (2017-03-28)
Essentials The role of platelet P2Y Background P2Y
The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
商品
电压门控钠通道存在于大多数可兴奋细胞膜中，在产生动作电位方面起着重要作用。
Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.
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