1170613-55-4
1170613-55-4 structure
- Name: A-967079
- Chemical Name: (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-penten-3-one Oxime
- CAS Number: 1170613-55-4
- Molecular Formula: C12H14FNO
- Molecular Weight: 207.244
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2018-12-03 09:17:16
- Modify Date: 2024-01-12 16:33:29
-
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
| Name | (1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-penten-3-one Oxime |
|---|---|
| Synonyms |
A967079 /A-967079
(1E,3E)-1-(4-Fluorophenyl)-2-methyl-1-penten-3-one oxime (1E,3E)-1-(4-fluorophenyl)-2-methylpent-1-en-3-one oxime (1E,3E)-1-(4-FLUOROPHENYL)-2-METHYL-1-PENTEN-3-ONEOXIME A-967079 |
| Description | A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS. |
|---|---|
| Related Catalog | |
| Target |
IC50: 67 nM (human TRPA1 receptor), 289 nM (rat TRPA1 receptor)[1] |
| In Vivo | Systemic injection of A-967079 (30 μmol/kg, i.v.) decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats. Similar to its actions in uninjured rats, administration of A-967079 (30 μmol/kg, i.v.) to complete Freund's adjuvant (CFA)-inflamed rats significantly reduces WDR neuronal responses to noxious pinch stimulation compared to baseline firing (p=0.0013, repeated-measures ANOVA) and the vehicle group (p=0.0001, two-way ANOVA). The maximum observed effect (61.1±10.97% decrease from baseline levels) on pinch-evoked activity in inflamed rats occur 35 min after injection. In contrast to uninjured rats, injection of A-967079 to CFA-inflamed rats also significantly (p=0.0004, and p=0.0001 for the repeated-measures and two-way ANOVA's, respectively) reduces responses of WDR neurons to 10-g von Frey hair stimulation. The maximal observed decrease in von Frey-evoked activity is 67.69±18.39% from baseline levels (35 min post-injection), and is thus comparable to the effects of A-967079 on pinch-evoked activity in inflamed rats[1]. |
| Animal Admin | Rats[1] Male Sprague-Dawley rats (250-400 g) are used for all experiments and are housed in a temperature controlled room with a 12/12-hr day/night cycle. Food and water are available ad libitum. Spontaneous and evoked neuronal activity is then measured 5, 15, 25, and 35 min after systemic injection of A-967079 (30 μmol/kg, i.v.) or vehicle (polyethylene glycol). The intravenous injection of A-967079 or vehicle is completed over a 6-7 min period. The i.v. dose of A-967079 is selected based on extrapolated plasma levels that are effective in behavioral studies[1]. |
| References |
| Density | 1.0±0.1 g/cm3 |
|---|---|
| Boiling Point | 324.4±34.0 °C at 760 mmHg |
| Molecular Formula | C12H14FNO |
| Molecular Weight | 207.244 |
| Flash Point | 150.0±25.7 °C |
| Exact Mass | 207.105942 |
| PSA | 32.59000 |
| LogP | 3.73 |
| Vapour Pressure | 0.0±0.7 mmHg at 25°C |
| Index of Refraction | 1.498 |
| Storage condition | 2-8℃ |
| Water Solubility | Very slightly soluble (0.19 g/L) (25 ºC) |
| RIDADR | NONH for all modes of transport |
|---|---|
| HS Code | 2928000090 |
| HS Code | 2928000090 |
|---|---|
| Summary | 2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0% |