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
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
A-803467, ≥98% (HPLC)
SMILES string
COc1cc(NC(=O)c2ccc(o2)-c3ccc(Cl)cc3)cc(OC)c1
InChI key
VHKBTPQDHDSBSP-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: >10 mg/mL
originator
Abbott
storage temp.
room temp
Quality Level
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相关类别
General description
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。
Biochem/physiol Actions
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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
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
Peripheral Receptor Targets for Analgesia: Novel Approaches to Pain Management (2009)
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
Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.
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。
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