DCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM.
| Molecular Weight | 427.36 |
| Formula | C22H28Cl2O4 |
| CAS Number | 82749-70-0 |
| Solubility (25°C) | DMSO 85 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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