所有图片(1)
About This Item
经验公式（希尔记法）:
C19H16NO4Cl
CAS号:
分子量:
357.79
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
检测方案
≥98% (HPLC)
形式
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
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。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
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
Peripheral Receptor Targets for Analgesia: Novel Approaches to Pain Management (2009)
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
Michael F Jarvis et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(20), 8520-8525 (2007-05-08)
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 contributes to experimental inflammatory and neuropathic pain. We report here the discovery of A-803467, a sodium channel
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.
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系技术服务部门