A 967079 |
Catalog No.GC11701
One-Click Copy Product Info
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Selective TRPA1 channel blocker
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1170613-55-4
Sample solution is provided at 25 µL, 10mM.
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A-967079 is an antagonist of transient receptor potential A1 (TRPA1) receptor with IC50 values of 289 nM and 67 nM at rat and human TRPA1 receptors, respectively [1].
There is a larger family of transient receptor potential (TRP) ion channels. In this family, there are TRPV, TRPM, TRPC, TRPN, TRPP and TRPML. TRPA1 is a part of this family and is expressed in small and medium-sized peptidergic primary afferent sensory neurons that also express TRPV1 [1].
Treatment with A-967079 attenuated Ca2+ signal in WT TG neurons and resulted in a further reduction in Trpv4-/- TG neurons in response to formalin. Treatment with A-967079 reduced the percentage of responsive cells from 27.7% to 15.8% when acutely blocking TRPA1 and to a mere 3.2% in Trpv4-/- TG neurons plus TRPA1 inhibitor [2].
Spontaneous activity of WDR neurons can indicate central sensitization and possibly non-evoked or ongoing pain. In uninjured and CFA-inflamed rats, systemic injection of A-967079 at 30 μmol/kg, i.v. made responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons decrease, following noxious pinch stimulation of the ipsilateral hind paw. Similarly in both OA and OA-sham rats, A-967079 decreased the responses of WDR neurons to high-intensity mechanical stimulation of the knee joint. Administration with A-967079 also reduced WDR neuronal responses to low-intensity mechanical stimulation (10 g von Frey hair) in CFA-inflamed rats, but not in uninjured rats. Additionally, A-967079 injection decreased the spontaneous activity of WDR neurons in CFA-inflamed rats, but not in uninjured, OA, and OA-sham animals [1].
References:
[1]. McGaraughty S, Chu KL, Perner RJ, et al. TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Molecular pain, 2010, 6(1): 1.
[2]. Chen Y, Kanju P, Fang Q, et al. TRPV4 is necessary for trigeminal irritant pain and functions as a cellular formalin receptor. PAIN, 2014, 155(12): 2662-2672.
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Animal experiment: |
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]. |
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References: [1]. McGaraughty S, et al. TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats. Mol Pain. 2010 Mar 5;6:14. |
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| Cas No. | 1170613-55-4 | SDF | |
| Chemical Name | (1Z,3E)-1-(4-fluorophenyl)-2-methylpent-1-en-3-one oxime | ||
| Canonical SMILES | FC1=CC=C(C=C1)/C=C(C)\C(CC)=N\O | ||
| Formula | C12H14FNO | M.Wt | 207.24 |
| Solubility | DMF: 20 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml,Ethanol: 20 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8253 mL | 24.1266 mL | 48.2532 mL |
| 5 mM | 965.1 μL | 4.8253 mL | 9.6506 mL |
| 10 mM | 482.5 μL | 2.4127 mL | 4.8253 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)