JNJ-303

Kv.1抑制剂(IC50=0.064µM)；选择性抑制INa、IKr、Ito、IK1和ICaL上的IK（IC50分别为3.3、12.6、11.1、>100和>10µM）；选择性抑制异源Kv7.1-KCNE1复合物(IC50=0.0784µM)，而1µM浓度下对Xenopus卵母细胞中的同源Kv7.1、Kv7.2或Kv1.5没有影响；在麻醉狗中分别以0.63和1.25mg/kg的剂量延长QT间期并诱发暂停依赖性TdP。An inhibitor of Kv.1 (IC50 = 0.064 µM); selective for inhibiting IKs over INa, IKr, Ito, IK1, and ICaL (IC50s =3.3, 12.6, 11.1, >100, and >10 µM, respectively); 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; prolongs the QT interval and also induces pause-dependent TdP in anesthetized dogs at 0.63 and 1.25 mg/kg, respectively.分子式C21H29ClN2O4S分子量441O=C(C(C)(C)OC(C=C1)=CC=C1Cl)N[C@@H]([C@@H]2C3)[C@H](C[C@@H]4C2)C[C@@]3(C4)N[S](C)(=O)=O