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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
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
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
Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad (2010)
The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
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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