PDE5 Inhibitor

Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

PDE5-IN-9 (Compound 59) is a PDE5 inhibitor (IC₅₀: 11.2 μM). PDE5-IN-9 shows interaction with Gln 817, Tyr 612, and Ala 767 amino acid residues. PDE5-IN-9 can be used for research of cardiovascular disease.

PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC₅₀ values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.

T-1032 is a selective phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ value of 1.0 nM. T-1032 shows relaxant effect on isolated rabbit corpus cavernosum. T-1032 can be used for the research of erectile dysfunction.

PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (K_D of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC₅₀s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research.

PDE5-IN-14 (Compound 14a) is a brain-penetrant competitive phosphodiesterase 5 (PDE5) inhibitor (IC₅₀=16.11 nM). PDE5-IN-14 is promising for research of Alzheimer’s disease (AD), cancer and cardiovascular diseases.

Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC₅₀ values of 48.8 μM and 477.5 μM, respectively.

CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD).

PDE5-IN-10 (compound 4b) is a potent PDE5 inhibitor with an IC₅₀ of 20 nM. PDE5-IN-10 improves in vitro microsomal stability (t_1/2 = 44.6 min) as well as excellent efficacy in restoring long-term potentiation. PDE5-IN-10 can be used for Alzheimer’s disease (AD) research.

1,3,5-Trihydroxy-4-prenylxanthone is a Na⁺/H⁺ exchange system inhibitor with a minimum inhibitory concentration of 10 μg/mL. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 3.0 μM. 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (HY-D1056)-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities.

FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the researches of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.

12-epi-Tadalafil is a PDE5 inhibitor (IC₅₀: 0.09 μM). 12-epi-Tadalafil can be used for research of cardiovascular diseases.

PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC₅₀ values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction.

Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC₅₀ values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.

PDE4-IN-1 is a PDE4 inhibitor with high potency (IC₅₀ : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.

TC-E 5005 is a potent and selective PDE10A inhibitor with IC₅₀ values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate.

PDE5-IN-5 (Compound 11) is a potent, selective phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 2.0 nM.

PDE5-IN-12 (compound 4h) is a potent phosphodiesterase-5 (PDE-5) inhibitor with an IC₅₀ of 22 nM. PDE5-IN-12 shows anti-proliferative effects against the aortic cell line.

PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC₅₀ of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.

PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia.