Adekalant, also known as H 345/52. is a new antiarrhythmic compound with low proarrhythmic activity. Adekalant concentration-dependently blocked HERG-carried currents with an IC50 of 230 nM. Adekalant preferentially bound to the open channel with unusually rapid kinetics and was trapped by channel closure. Voltage-independent behavior of Adekalant was observed during both square-pulse and action potential clamp protocols. It is proposed that block of I(Kr) is the principal mechanism by which Adekalant delays repolarization in human myocardium. Adekalant blocks I(Kr) with high potency and I(Ca) with somewhat lower potency and was found to delay ventricular repolarization without substantially increasing temporal or spatial dispersion and without inducing early after-depolarizations or TdP.
MedKoo Cat#: 126841
Name: Adekalant
CAS#: 227940-00-3 (free base)
Chemical Formula: C22H31N3O4
Exact Mass: 401.2315
Molecular Weight: 401.51
Elemental Analysis: C, 65.81; H, 7.78; N, 10.47; O, 15.94
The following data is based on the product molecular weight 401.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
