Nifekalant (hydrochloride)

Nifekalant is a class III antiarrhythmic agent. It inhibits the rapidly activating delayed rectifier potassium channel (IKr, IC50 = 10 µM) and prolongs cardiac action potential duration (APD) in isolated dog Purkinje fibers when used at concentrations of 1 and 3 µg/ml. Nifekalant (3 mg/kg) inhibits arrhythmias induced by programmed electrical stimulation (PES) in dogs post myocardial infarction. It increases atrial and ventricular effective refractory periods (ERPs) in anesthetized dogs. Nifekalant also inhibits human multidrug and toxin extrusion (MATE) transporter 1 (MATE1, IC50 = 6.5 µM). Formulations containing nifekalant have been used in the treatment of arrhythmias and ventricular tachycardia.Formal Name: 6-[[2-[(2-hydroxyethyl)[3-(4-nitrophenyl)propyl]amino]ethyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione, monohydrochloride. CAS Number: 130656-51-8. Synonyms: MS-551. Molecular Formula: C19H27N5O5 . HCl. Formula Weight: 441.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 267 nm. SMILES: OCCN(CCNC1=CC(N(C)C(N1C)=O)=O)CCCC2=CC=C([N+]([O-])=O)C=C2.Cl. InChi Code: InChI=1S/C19H27N5O5.ClH/c1-21-17(14-18(26)22(2)19(21)27)20-9-11-23(12-13-25)10-3-4-15-5-7-16(8-6-15)24(28)29,/h5-8,14,20,25H,3-4,9-13H2,1-2H3,1H. InChi Key: YPVGGQKNWAKOPX-UHFFFAOYSA-N.