PF-03882845

PF-03882845 is a non-steroidal mineralocorticoid receptor antagonist (IC50 = 26 nM). It is selective for the mineralocorticoid receptor over the androgen, glucocorticoid, and progesterone receptors in reporter assays using Huh7 cells (IC50s = >10,000, >10,000, and 1,880 nM, respectively). PF-03882845 (40 and 100 mg/kg) prevents blood pressure increases and kidney damage in rats fed a high-salt diet. It inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) guanine-N7 methyltransferase in a homogenous time-resolved fluorescence (HTRF) assay (IC50 = 1.1 µM) and reduces SARS-CoV-2 infectivity in Vero E6 cells (EC50 = 10.97 µM). PF-03882845 also inhibits Zika virus NS2B-NS3 protease in a reporter assay (IC50 = 1 µM) and reduces Zika virus infectivity in neural stem cells generated from human induced pluripotent stem cells (iPSCs, IC50 = 10.8 µM).. SMILES: ClC1=CC(N2[C@@H](C3CCCC3)[C@H]4CCC5=CC(C(O)=O)=CC=C5C4=N2)=CC=C1C#N. InChi Code: InChI=1S/C24H22ClN3O2/c25-21-12-18(8-5-17(21)13-26)28-23(14-3-1-2-4-14)20-10-6-15-11-16(24(29)30)7-9-19(15)22(20)27-28/h5,7-9,11-12,14,20,23H,1-4,6,10H2,(H,29,30)/t20-,23-/m0/s1. InChi Key: XNULRSOGWPFPBL-REWPJTCUSA-N