LUF7346 is a Kv11.1 (hERG) allosteric modulator that prevents proarrhythmic effects caused by hERG blockers in rat ventricular myocyte cultures. LUF7346 reduces Kv11.1 (ERG) affinity toward known Kv11.1 channel blockers dofetilide (Ki for hERG = 4.8 nM without and 12 nM with 10 μM LUF7346) and astemizole (Ki for for hERG = 1.3 nM without and 5.3 nM with 10 μM LUF7346) and effectively suppresses astemizole-induced arrhythmogenic events in a dose-dependent manner among Long-QT syndrome/LQTS (LQT1, JLNS, LQT2) and control isogenic human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). LUF7346 is shown to slow IKr deactivation and positively shifts IKr inactivation among LQTS and control isogenic hiPSC-CMs without affecting KCNQ1/KCNE1-dependent IKs or L-type calcium current ICaL.
| Molecular Weight | 411.25 |
| Formula | C20H15BrN2O3 |
| CAS Number | 1821638-40-7 |
| Solubility (25°C) | DMSO: 10 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.
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