pde1-in-3

PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1).

PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM and is applicable in pulmonary arterial hypertension research. It demonstrates high selectivity for its target compared to PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11, and it possesses oral bioavailability.

Olprinone Hydrochloride, also known as Loprinone, is a phosphodiesterase (PDE) 3 potent inhibitor, exhibiting IC50 values of 150, 100, 0.35, and 14 μM for PDE1, PDE2, PDE3, and PDE4, respectively. It is utilized in heart failure research for its positive inotropic and vasodilative properties. It also exhibits anti-inflammatory activity [1] [2].

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

Phosphodiesterase (PDE), an enzyme capable of catalyzing the hydrolysis of the 3' ring phosphate bond in cyclic nucleotides, plays a crucial role in biochemical research and acts as a vital regulator in signal transduction processes involving the second messenger molecules cAMP and cGMP. Distinguished by their specificity to cyclic nucleotides, PDEs are categorized into different types ranging from PDE1 to PDE11, presenting potential significance in the study and treatment of various diseases [1].