pde10a

PDE10A-IN-8 is a potent inhibitor of PDE10A.

Compound 8a (PDE10A-IN-3) serves as an inhibitor of phosphodiesterase 10A (PDE10A) and is utilized in schizophrenia research [1].

N-Methylbenzamide is a potent inhibitor of phosphodiesterase 10A (PDE10A) with demonstrated anti-cancer activity.

MK-8189 is a potent and selective pyrimidine PDE10A inhibitor, Ki = 0.029nM, with excellent PDE (phosphodiesterase) selectivity for the treatment of schizophrenia.

PQ-10 (A-844337) is a PDE-10 inhibitor. PQ-10 induces brain glucose metabolism patterns, which may be a potential translational biomarker.

THPP-1 is a potent and orally bioavailable inhibitor of PDE10A(Ki of 1 nM and 1.3 nM for human and rat PDE10A, respectively).

PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5 (IC50 of 0.31 nM).

AMG580 is a selective PDE10A antagonist exhibiting sub-nanomolar affinity towards PDE10A in rats, primates, and humans. It is utilized in research as a non-invasive radiotracer.

PDE4-IN-12 is a potent and safe ubiquitous PDE4 inhibitor with an IC50 of 3.5 nM (SI: 2.71) and also acts on PDE7 with an IC50 of 15 nM (SI: 4.27).

Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs.

PDM-042 is a potent and selective orally active phosphodiesterase 10A (PDE10A) inhibitor, demonstrating strong inhibitory activities for human and rat PDE10A with IC50 values below 1 nM and over 1000-fold selectivity against other phosphodiesterases. PDM-042 can be used for schizophrenia research [1].

MT-3014 is a potent, highly selective, and brain-penetrant inhibitor of phosphodiesterase 10A (PDE 10A), with IC50 values of 0.062 nM for human PDE 10A and 0.09 nM for bovine PDE 10A.

WAY-620445 is an active molecule [1]. It is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 1.8 nM. This compound has demonstrated efficacy in preclinical models of psychosis and is being explored as a potential therapeutic agent for schizophrenia.

Gemlapodect (RO554965), a phosphodiesterase 10A (PDE10A) inhibitor, is utilized in schizophrenia research.

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).

PDE10A inhibitor

(1R,2R)-MK-8189 is an isomer of MK-8189 and can be used for biochemistry experoments. MK-8189 is a potent and selective pyrimidine PDE10A inhibitor.

5,7-Dichloropyrazolo[1,5-a]pyrimidine (fragment 5) is an inhibitor of the enzyme phosphodiesterase 10A (PDE10A) with a Ki value of 24 μM. This compound can be employed in research related to schizophrenia.

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.

Mardepodect hydrochloride (Mardepodect HCl) is an orally active, selective and potent inhibitor of PDE10A that crosses the blood-brain barrier (IC50: 0.37 nM).Mardepodect hydrochloride up-regulates the expression of proteins encoding specific growth and transcription factors, cell signalling molecules and cell surface proteins. Mardepodect hydrochloride upregulates genes encoding specific growth factors, transcription factors, cell signalling molecules, and cell surface proteins, while downregulating a broad spectrum of cell cycle and apoptosis-related genes.

HPP-2 is a novel phosphodiesterase 10A (PDE10A) inhibitor used to treat schizophrenia.

MP-10 succinate is a potent and specific inhibitor of PDE10A.

THPP-4 inhibits phosphodiesterase 10A (PDE10A).

AMG 579 is an efficacious and selective inhibitor of PDE10A (IC50 = 0.1 nM).