pde1a

Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.

Gisadenafil besylate (UK 369003-26) is a potent and orally active PDE5 inhibitor (IC50=1.23 nM), 100 times more selective for PDE5 than PDE6, for the study of lower urinary tract symptoms associated with benign prostatic hyperplasia.

TAK-915 is a potent, selective, and brain-penetrant phosphodiesterase 2A (PDE2A) inhibitor (IC50: 0.61 nM) with >4100-fold selectivity for PDE2A over PDE1A.

PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.

ITI-214 free base, a picomolar PDE1 inhibitor (Ki = 58 pM), exhibits excellent selectivity against other PDE family members and a range of enzymes, receptors, transporters, and ion channels.

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

PDE1-IN-8 (Compound 3f) acts as an inhibitor of PDE1, with an IC50 of 11 nM. It hinders cAMP and cGMP signaling pathways, impeding the differentiation and proliferation of cells into myofibroblasts, and demonstrates antifibrotic effects in the Bleomycin-induced rat model of pulmonary fibrosis.

DSR-141562 is a new compound that can be taken orally and has a specific ability to inhibit phosphodiesterase 1 (PDE1) in the brain. This compound exhibits a preference for inhibiting human PDE1B, with an IC50 value of 43.9 nM. It also shows moderate inhibition of human PDE1A (IC50 = 97.6 nM) and PDE1C (IC50 = 431.8 nM). DSR-141562 is particularly useful in the study of positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia.

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).

Osoresnontrine is a potent and selective inhibitor of PDE9A (IC50 of 52 nM),and can be used in the research of memory.

Tovinontrine (IMR-687) (IMR-687) is a potent and selective inhibitor of phosphodiesterase-9 (PDE9), designed to target sickle cell disease treatment. It exhibits high efficacy, with IC 50 values of 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively [1].