PDE5 Inhibitor

Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC₅₀ of 0.074 nM) inhibitor, is used for sexual enhancement study.

T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC₅₀=0.23 nM). T-0156 inhibits PDE6 (IC₅₀=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC₅₀>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.

PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC₅₀ values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease.

Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM respectively, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^-.

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.

TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction.

PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC₅₀ of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC₅₀s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.

ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3.

PDE4-IN-30 is a selective PDE4 inhibitor with an IC₅₀ of 2.7 nM for PED4D2, targeting PDE4 through halogen bonding and metal coordination. PDE4-IN-30 exhibits at least 67-fold selectivity for other PDE subfamilies. PDE4-IN-30 can be used for the research of idiopathic pulmonary fibrosis.

OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC₅₀ values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC₅₀s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.

Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC₅₀ of 0.074 nM) inhibitor, is used for sexual enhancement study.

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

PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC₅₀ of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC₅₀ of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC₅₀=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.

PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC₅₀ of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.

(R)-Xanthoanthrafil is a phosphodiesterase-5 (PDE5) inhibitor. (R)-Xanthoanthrafil selectively inhibits PDE5, increasing cyclic guanosine monophosphate (cGMP) levels, leading to smooth muscle relaxation and promoting penile erection. (R)-Xanthoanthrafil can be used to study erectile dysfunction.

BMS-341400 is an orally active selective phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ value of 0.3 nM. BMS-341400 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 can be used to study erectile dysfunction.

PF-03049423 (Compound PF-5) free base 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 free base can be used for the research of acute ischaemic stroke.

PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC₅₀s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs).

CM-545, the cis-isomer of CM-414 (HY-119316), is a dual inhibitor of PDE5, HDAC1, HDAC2, HDAC3, and HDAC6 with pIC₅₀ values of 7.47, 6.65, 6.14, 6.55, and 6.84, repectively.