1. Membrane Transporter/Ion Channel
  2. TRP Channel

A-967079 

Cat. No.: HY-108463 Purity: 98.66%
Handling Instructions

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.

For research use only. We do not sell to patients.

A-967079 Chemical Structure

A-967079 Chemical Structure

CAS No. : 1170613-55-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 410 In-stock
Estimated Time of Arrival: December 31
100 mg USD 730 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & 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].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (603.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8253 mL 24.1266 mL 48.2532 mL
5 mM 0.9651 mL 4.8253 mL 9.6506 mL
10 mM 0.4825 mL 2.4127 mL 4.8253 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

207.24

Formula

C₁₂H₁₄FNO

CAS No.

1170613-55-4

SMILES

CCC(/C(C)=C/C1=CC=C(F)C=C1)=N\O.[E].[E]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
A-967079
Cat. No.:
HY-108463
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A-967079

Cat. No.: HY-108463