852146-73-7

KR-32568 is a sodium/hydrogen exchanger-1 (NHE-1) inhibitor with an IC50 of 230 nM. KR-32568 has cardioprotective effects[1][2].

Sodium/hydrogen exchanger-1 (NHE-1) inhibitor; IC50 = 0.23 μM; inhibited NHE-1-mediated rabbit platelet swelling; in anesthetized ratsreduced infarct size from 67% (control) to 43% ( at 0.1 mg/kg) and 24% ( at 1.0 mg/kg); reduced number of ventricular premature beats from 530 to 266 ( at 0.1 mg/kg) and 115 ( at 1.0 mg/kg); reduced ventricular fibrillation incidence from 17 to 8 (0.1 mg/kg) and 0 (1.0 mg/kg); implications for research and treatment of myocardial ischemic diseases.

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[1] Hui-Yul Roh, et al. Cardioprotective effects of [5-(2-methyl-5-fluorophenyl)furan-2-ylcarbonyl]guanidine (KR-32568) in an anesthetized rat model of ischemia and reperfusion heart injury. Pharmacology. 2005 Dec;75(1):37-44. DOI:10.1159/000086192
[2] Sunkyung Lee, et al. (5-Arylfuran-2-ylcarbonyl)guanidines as cardioprotectives through the inhibition of Na+/H+ exchanger isoform-1. J Med Chem. 2005 Apr 21;48(8):2882-91. DOI:10.1021/jm0492305