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经验公式(希尔记法):
C12H14FNO
化学文摘社编号:
分子量:
207.24
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.25
MDL number:
产品名称
A-967079, ≥98% (HPLC)
SMILES string
CCC(=N/O)\C(C)=C\c1ccc(F)cc1
InChI key
HKROEBDHHKMNBZ-CHBKHGQFSA-N
InChI
1S/C12H14FNO/c1-3-12(14-15)9(2)8-10-4-6-11(13)7-5-10/h4-8,15H,3H2,1-2H3/b9-8+,14-12+
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥12 mg/mL
originator
Abbott
storage temp.
2-8°C
Quality Level
相关类别
General description
A-967079可防止神经性和炎症性疼痛。它会降低神经损伤引起的冷痛觉超敏。
Application
A-967079可用于阻断miR-711诱导TRPA1(瞬时受体电位阳离子通道亚家族A成员1)通道。
Biochem/physiol Actions
A-967079 是一种有效的、选择性瞬时受体电位锚蛋白 1(TRPA1)拮抗剂,在人和大鼠 TRPA1 受体上的 Ic50′s50′s 分别为 67 nM 和 289 nM,在其他 89 个测试的 TRP 通道或 G 蛋白偶联受体、酶、转运蛋白和离子通道中活性极小或没有活性。A-967079 阻断人和大鼠细胞系中的 TRPA1 激活,并且可以减少宽动态范围(WDR)和伤害特异性(NS)神经元对高强度机械刺激的反应。
TRPA1 素受体拮抗剂
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
miRNA-711 binds and activates TRPA1 extracellularly to evoke acute and chronic pruritus
Han Q, et al.
Neuron, 99(3), 449-463 (2018)
Molecular basis determining inhibition/activation of nociceptive receptor TRPA1: a single amino acid dictates species-specific actions of the most potent mammalian trpa1 antagonists
Banzawa N, et al.
The Journal of biological chemistry, jbc-M114 (2014)
Molecular basis determining inhibition/activation of nociceptive receptor TRPA1: a single amino acid dictates species-specific actions of the most potent mammalian trpa1 antagonists
Banzawa N, et al.
Test, jbc-M114 (2014)
Molecular basis determining inhibition/activation of nociceptive receptor TRPA1: a single amino acid dictates species-specific actions of the most potent mammalian trpa1 antagonists
Banzawa N, et al.
The Journal of Biological Chemistry, jbc-M114 (2014)
Steve McGaraughty et al.
Molecular pain, 6, 14-14 (2010-03-09)
There is growing evidence supporting a role for TRPA1 receptors in the neurotransmission of peripheral mechanical stimulation. In order to enhance understanding of TRPA1 contributions to mechanotransmission, we examined the effects a selective TRPA1 receptor antagonist, A-967079, on spinal neuronal
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