Praliciguat

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase (sGC) activator. Praliciguat can increases cGMP via the nitric oxide (NO)-sGC pathway. Praliciguat can inhibit the expression of proinflammatory cytokines and inhibit apoptosis. Praliciguat can promote vasodilation. Praliciguat can be used for the researches of metabolic disease and cardiovascular disease, such as hypertension, diabetes and heart failure^[1][2][3]. IC50 & Target:EC50: 197 nM (sGC)^[1] In Vitro:Praliciguat stimulates soluble guanylate cyclase in HEK-293 cells with an EC₅₀ of 197 nM^[1].
Praliciguat demonstrates concentration-dependent relaxation of pre-contracted subcutaneous resistance arteries (EC₅₀ = 34.7 nM)^[1].
Praliciguat (10 μM, 48 h) inhibits the expression of proinflammatory cytokines and secretion of monocyte chemoattractant protein 1 in TNF-α-challenged proximal tubular epithelial cells (RPTC)^[2].
Praliciguat (1-10 μM, 48 h) inhibits TGF-β-mediated apoptosis in RPTC^[2].
In Vivo:Praliciguat (1 mg/kg, p.o.) reduces arterial pressure (MAP) in normotensive and hypertensive rats^[1].
Praliciguat (1-10 mg/kg, p.o.) attenuates proteinuria in obese ZSF1 rats model of diabetic nephropathy^[2].
Praliciguat (1-10 mg/kg, p.o., daily for 2-7 weeks) attenuates inflammation, fibrosis, and end-organ damage in the Dahl rats model of cardiorenal failure^[3].