BI 689648 (C09-1113-776)

BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC 50 s of 310 and 2.1 nM, respectively.In VitroCompare with the FADs and LCI699, BI 689648 is highly selective in vitro , providing an IC 50 for CYP11B2 of 2.1 nM and a selectivity factor of 149 over CYP11B1. FAD286, by comparison, shows a similar IC 50 for CYP11B2 (2.5 nM); however, its greater potency against CYP11B1 (94 nM) results in a comparatively modest selectivity factor of 38, approximately 4-fold less than BI 689648. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAfter oral administration in cyno monkeys, BI 689648 (5 mg/kg) exhibits a peak plasma concentration of ~500 nM. For BI 689648 (aldosterone EC 50 =2 nM), appreciable changes in 11-DOC are only noted at plasma concentrations >2000 nM or >1000-fold its aldosterone EC 50 while FAD286 shows a window of ~100-fold. BI 689648 exhibits minimal impact on 11-DC and only at very high plasma concentrations (~10 μM) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 310 nM (CYP11B1), 2.1 nM (CYP11B2). Specification: 0.99 Molecular Formula: C16H18N4O2 Molecular Weight: 298.34 PubChem CID: 86305663 Isomeric SMILES: COCC1=CC(=CN=C1)C2=CC3=C(N=C2)N(CCC3)C(=O)N