A2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception.
| Molecular Weight | 351.7 |
| Formula | C15H21Cl3N2O |
| CAS Number | 861038-72-4 |
| Solubility (25°C) | DMSO 70 mg/mL Water 70 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.
| Related Potassium Channel Products |
|---|
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NPBA is a potassium K2P channel TASK-3 (KCNK9) agonist and a tandem pore domain weak inward rectifier K+ channel (TWIK2) channel blocker. In addition, NPBA inhibits the activation of NLRP3 inflammasome in macrophages. |
| BeKm-1
BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. |
| Apamin
Apamin (Apamine) is a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. |
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| Iberiotoxin
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