ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.
|Solubility (25°C)||DMSO 94 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitive K+ channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects.
Isopimaric acid is a potent opener of large conductance calcium activated K+ (BK) channels.
Dimethyl L-glutamate (Dimethyl glutamate) can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division.
Iberiotoxin TFA is a toxin isolated from Buthus tamulus venom and is also a selective, high-affinity blocker of the large conductance calcium-activated potassium channel (BKCa) with a Kd of approximately 1 nM.
Scyllatoxin (Leiurotoxin I) is a peptide toxin, it can be isolated from the venom of the scorpion (Leiurus quinquestriatus hebraeus). Scyllatoxin is a blocker of small-conductance KCa (SK) channel. Scyllatoxin enhances both norepinephrine (NE) and epinephrine (Epi) release in vivo.
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