Potassium channel blocker. Antimalarial, anticholinergic, antihypertensive, and hypoglycemic agent; alkaloid originally isolated from the Cinchona family of South American trees. Inhibits mitochondrial ATP-regulated potassium channel. Used to study the metabolism of biocrystalized heme, hemozoin, in malarial parasites and to study the toxicity of heme (FP)-complexes.
| Molecular Weight | 391.47 |
| Formula | C20H24N2O2 · 0.5H2O4S · H2O |
| CAS Number | 207671-44-1 |
| Solubility (25°C) | Water: slightly soluble 1.2 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
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. |
| Phe-Met-Arg-Phe amide trifluoroacetate
Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K+ current, with ED50 of 23 nM in the peptidergic caudodorsal neurons. |
| Iberiotoxin
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. |
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