BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.1 It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.2 It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.1 BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.2
1.Huber, J.D., Bentzien, J., Boyer, S.J., et al.Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the ratJ. Med. Chem.55(16)7114-7140(2012) 2.Kili?, A., Huang, C.X., Rajapurohitam, V., et al.Early and transient sodium-hydrogen exchanger isoform 1 inhibition attenuates subsequent cardiac hypertrophy and heart failure following coronary artery ligationJ. Pharmacol. Exp. Ther.351(3)492-499(2014)