PDE5 Inhibitor

PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC₅₀ values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.

PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC₅₀ of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model.

BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor. BL-122 can increase the level of cGMP in the tissue, promote the expression of nitric oxide (NO), and mediate the relaxation of smooth muscle. BL-122 can be used for the researches of inflammation, immunology and cardiovascular disease, such as asthma and hypertension.

UK 343664 is a potent, orally active and selective PDE5 inhibitor. UK 343664 partially reverses Thromboxane-induced pulmonary hypertension.

N-Desethyl-N-methyl vardenafil (Demethyl-vardenafil), an analog of Vardenafil (HY-B0442), is a PDE5 inhibitor with an IC₅₀ value of 0.14 μM.

Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, with an IC₅₀ of 3.95 ng/mL. Xanthoanthrafil can be used for the research of erectile dysfunction.

SCH 51866 is a potent, selective and orally active inhibitor of PDE1 (IC₅₀=70 nM) and PDE5 (IC₅₀=60 nM). SCH 51866 inhibits collagen-induced aggregation of human washed platelets (IC₅₀=10 μM), prevents neointimal formation in balloon catheter-injured carotid arteries of spontaneously hypertensive rats (SHR), and reduces blood pressure in SHR. SCH 51866 can be used in the study of hypertension.

UK-371800 is a highly selective PDE5 inhibitor (IC₅₀ = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein.

UK 357903 is a selective inhibitor for phosphodiesterase 5 (PDE5), with IC₅₀s of 1.7 and 714 nM, for PDE5 and PDE6. UK 357903 exhibits vasodilatory effects on the mesenteric and hindlimb vascular beds, and is potential for ameliorating erectile dysfunction.

P2Y12/PDE5-IN-1 (Compound 10) is a dual-target inhibitor of P2Y12 (IC₅₀ = 0.271 μg/mL) and PDE5 (IC₅₀ = 0.154 μg/mL). P2Y12/PDE5-IN-1 can be used for research on anti-thrombosis and vasodilation.

JNJ-10258859 is a potent and selective phosphodiesterase type 5 inhibitor, with a K_i of 0.23 nM. JNJ-10258859 can be used for erectile dysfunction research.

BMS-341400 mesylate is a selective phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ value of 0.3 nM. BMS-341400 mesylate reduces the degradation of cyclic guanosine monophosphate (cGMP), thereby enhancing nitric oxide (NO)-mediated relaxation of the smooth muscle of the corpus cavernosum and promoting erection. BMS-341400 mesylate can be used to study erectile dysfunction.