JNJ-303

JNJ-303 is an inhibitor of voltage-gated potassium channel Kv7.1 (IC50 = 0.064 µM). 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. 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.Formal Name: 2-(4-chlorophenoxy)-2-methyl-N-[5-[(methylsulfonyl)amino]tricyclo[3.3.1.13,7]dec-2-yl]-propanamide, stereoisomer. CAS Number: 878489-28-2. Molecular Formula: C21H29ClN2O4S. Formula Weight: 441.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, Ethanol: insol, PBS (pH 7.2): insol. lambdamax: 225 nm. SMILES: O=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. InChi Code: InChI=1S/C21H29ClN2O4S/c1-20(2,28-17-6-4-16(22)5-7-17)19(25)23-18-14-8-13-9-15(18)12-21(10-13,11-14)24-29(3,26)27/h4-7,13-15,18,24H,8-12H2,1-3H3,(H,23,25)/t13-,14-,15+,18-,21-. InChi Key: OSGIRCJRKSAODN-HPMFMUNCSA-N.