Fimasartan

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1^[1][2][3]. IC50 & Target:Inducible nitric oxide synthase (iNOS) and NLRP3^[1][2] In Vitro:Fimasartan (62.5, 125 and 250 µM; 1 h) inhibits NO production and the expression of inducible nitric oxide synthase in LPS(HY-D1056)-induced RAW264.7 macrophages^[1].
Fimasartan (250 µM; 1 h) decreases the activation of NF-κB and activator protein 1 in LPS(HY-D1056)-induced RAW264.7 macrophages^[1].
Fimasartan (30 ng/mL; 6 h) inhibits the activation of the NLRP3 inflammatome in a hemolysate -induced microglia model simulating cerebral hemorrhage^[2]. In Vivo:Fimasartan (0.5 mg/kg; Oral administration; 33 days) ameliorates NLRP3 inflammasome-mediated neuroinflammation and brain injury in a rat model of cerebral hemorrhage^[2].
Fimasartan (0.03-3 mg/kg; Oral administration/Intravenous injection; 3-24 h) has antihypertensive effect in hypertensive rats^[3].