A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively). Displays 1000-fold selectivity for TRPA1 over other TRP channels, and is >150-fold selective over 75 other ion channels, enzymes and G-protein-coupled receptors. Exhibits analgesic effects in a rat osteoarthritic pain model.
| Molecular Weight | 207.24 |
| Formula | C12H14FNO |
| CAS Number | 1170613-55-4 |
| Solubility (25°C) | DMSO 20.72 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Jianhua Zhao, et al. Irritant-evoked activation and calcium modulation of the TRPA1 receptor
[3] Stefan Heber, et al. A Human TRPA1-Specific Pain Model
[5] Ari Koivisto, et al. TRPA1: a transducer and amplifier of pain and inflammation
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