| Bioactivity | BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury[1]. | ||||||||||||
| Target | IC50: 6 nM (NHE1 in intracellular pH recovery assay), 31 nM (NHE1 in human platelet swelling assay) | ||||||||||||
| Name | BI-9627 | ||||||||||||
| CAS | 1204329-34-9 | ||||||||||||
| Formula | C16H19F3N4O2 | ||||||||||||
| Molar Mass | 356.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Huber JD, et al. Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitableprofile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat. J Med Chem. 20 |