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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.
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)
Minagi Mukaiyama et al.
Journal of biochemistry, 168(4), 407-415 (2020-05-20)
Activation of the transient receptor potential A1 channel (TRPA1) by electrophilic agonists was reported to induce the opening of tight junctions (TJs). Because compounds that increase TJ permeability can be paracellular permeability enhancers, we investigated the effect of non-electrophilic TRPA1
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