898563-00-3

898563-00-3 structure

Name: TP-10
Chemical Name: 2-({4-[4-(4-Pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]p henoxy}methyl)quinoline
CAS Number: 898563-00-3
Molecular Formula: C₂₆H₁₉F₃N₄O
Molecular Weight: 460.45000
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2019-01-15 10:47:41
Modify Date: 2024-01-03 21:08:01
TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM.IC50 value: 0.8 nM [1]Target: PDE10ATP-10 has extremely potent PDE10A inhibitory activity and highselectivity against other PDEs, and be active in the mouse behavioral model for positive symptoms. TP-10 demonstrats good in vitro and in vivo activity, the intrinsic clearance (CLint) of these compounds in mouse liver microsomes (MLM) was extremely high in assay (CLint>1000 mL/min/kg). [1]

Name	2-({4-[4-(4-Pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]p henoxy}methyl)quinoline
Synonyms	TP-10

Description	TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM.IC50 value: 0.8 nM [1]Target: PDE10ATP-10 has extremely potent PDE10A inhibitory activity and highselectivity against other PDEs, and be active in the mouse behavioral model for positive symptoms. TP-10 demonstrats good in vitro and in vivo activity, the intrinsic clearance (CLint) of these compounds in mouse liver microsomes (MLM) was extremely high in assay (CLint>1000 mL/min/kg). [1]
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Cardiovascular Disease
References	[1]. Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213. [2]. Verhoest PR, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem