推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to tan
溶解性
DMSO: ≥12 mg/mL
创始人
Abbott
储存温度
2-8°C
SMILES字符串
CCC(=N/O)\C(C)=C\c1ccc(F)cc1
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+
InChI key
HKROEBDHHKMNBZ-CHBKHGQFSA-N
一般描述
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。
应用
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。
生化/生理作用
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。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Molecular basis determining inhibition/activation of nociceptive receptor TRPA1: a single amino acid dictates species-specific actions of the most potent mammalian trpa1 antagonists
The Journal of biological chemistry, jbc-M114 (2014)
miRNA-711 binds and activates TRPA1 extracellularly to evoke acute and chronic pruritus
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
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
The Journal of Biological Chemistry, jbc-M114 (2014)
Journal of pain research, 11, 51-60 (2018-01-19)
Transient receptor potential ankyrin 1 (TRPA1) is a non-selective cation channel expressed by a subset of nociceptive neurons that acts as a multimodal receptor. Its activity contributes to modulate nociceptive transmission in acute inflammatory pain. However, the role of this
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