| Identification | Back Directory | [Name]
A 967079 | [CAS]
1170613-55-4 | [Synonyms]
A 967079
(1E,3E)-1-(4-Fluorophenyl)-2-Methyl-1-penten-3-one oxiMe
(1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime
1-Penten-3-one, 1-(4-fluorophenyl)-2-methyl-, oxime, (1E,3E)-
TRP Channel,inhibit,Transient receptor potential channels,A 967079,Inhibitor,A-967079,A967079 | [Molecular Formula]
C12H14FNO | [MDL Number]
MFCD20488058 | [MOL File]
1170613-55-4.mol | [Molecular Weight]
207.24 |
| Chemical Properties | Back Directory | [Boiling point ]
324.4±34.0 °C(Predicted) | [density ]
1.03±0.1 g/cm3 (20 ºC 760 Torr) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥12mg/mL | [form ]
powder | [pka]
12.23±0.40(Predicted) | [color ]
white to tan | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months | [InChI]
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+ | [InChIKey]
HKROEBDHHKMNBZ-CHBKHGQFSA-N | [SMILES]
C(/C1=CC=C(F)C=C1)=C(/C)\C(=N\O)\CC |
| Hazard Information | Back Directory | [Description]
A-967079 (1170613-55-4) is a TRPA1 blocker. Active in rat models.1 Cell permeable | [Uses]
(1E,3E)- 1-(4-Fluorophenyl)-2-methyl-1-penten-3-one Oxime is a transient receptor potential ankyrin 1 (TRPA1) antagonist and has been investigated as potential analgesic drug for the treatment of chronic pain. | [Uses]
A-967079 has been used in blocking miR-711-induced TRPA1 (transient receptor potential cation channel subfamily A member 1) channel. | [General Description]
A-967079 prevents neuropathic and inflammatory pain. It reduces cold allodynia, which is produced by nerve injury. | [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. | [storage]
Store at -20°C | [Advantages]
(1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-pentene-3-one oxime (A-967079) has shown impressive efficacy as an antagonist to TRPA1 and has multiple advantages over other compounds, including high selectivity, potency, and oral bioavailability. A-967079 has IC50 values of 67 and 289 nM for human and rat TRPA1 receptors, respectively. It displays 1000-fold selectivity for TRPA1 over other TRP channels, and >150-fold selectivity for over 75 other ion channels, enzymes and G-protein-coupled receptors. Oral administration of A-967079 in rats produced robust bioavailability and analgesic efficacy for TIH-induced pain response (i.e., sneezing, tearing, coughing, etc.) and osteoarthritic pain. Intravenous injection of A-967079 has shown to decrease the reactive gas response of wide dynamic range neurons (i.e., a second-order neuron that responds to more than one type of stimulus) and pain specific-neurons. Aditionally, A-967079 produces no known locomotor or cardiovascular effects, a common side effect of other TRP antagonists[2]. | [References]
1) McGaraughty et al. (2010), TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats; Mol. Pain, 6 14. |
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