SML0085
A-967079
≥98% (HPLC), Selective Transient Receptor Potential Anykrin 1 (TRPA1) antagonist, powder
Synonym(s):
(1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-penten-3-one oxime
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About This Item
Empirical Formula (Hill Notation):
C12H14FNO
CAS Number:
Molecular Weight:
207.24
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.25
MDL number:
Product Name
A-967079, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥12 mg/mL
originator
Abbott
storage temp.
2-8°C
SMILES string
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
Related Categories
General description
A-967079 prevents neuropathic and inflammatory pain. It reduces cold allodynia, which is produced by nerve injury.
Application
A-967079 has been used in blocking miR-711-induced TRPA1 (transient receptor potential cation channel subfamily A member 1) channel.
Biochem/physiol Actions
A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
TRPA1 receptor antagonist
Features and Benefits
This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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.
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)
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)
Jun Chen et al.
Pain, 152(5), 1165-1172 (2011-03-16)
Despite the increasing interest in TRPA1 channel as a pain target, its role in cold sensation and body temperature regulation is not clear; the efficacy and particularly side effects resulting from channel blockade remain poorly understood. Here we use a
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML0085-5MG | 04061833236505 |
| SML0085-25MG | 04061837076763 |
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