产品描述:
JNJ-303 is an inhibitor of voltage-gated potassium channel Kv7.1 (IC50 = 0.064 µM).{69120} It is selective for inhibiting Kv7.1 currents (IKs) over INa, IKr, Ito, IK1, and ICaL (IC50s =3.3, 12.6, 11.1, >100, and >10 µM, respectively). It selectively inhibits the heteromeric Kv7.1-KCNE1 complex (IC50 = 0.0784 µM) with no effect on homomeric Kv7.1, Kv7.2, or Kv1.5 in Xenopus oocytes at 1 µM.{69121} JNJ-303 prolongs the QT interval and also induces pause-dependent torsade de pointes (TdP) in anesthetized dogs when used at doses of 0.63 and 1.25 mg/kg, respectively.{69120}