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898563-00-3

898563-00-3 Structure

898563-00-3 Structure
IdentificationBack Directory
[Name]

2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline
[CAS]

898563-00-3
[Synonyms]

TP-10
2-[[4-[4-pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline
2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline
2-({4-[4-(4-Pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]p henoxy}methyl)quinoline
Quinoline, 2-[[4-[4-(4-pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]phenoxy]methyl]-
schizophrenia,U-87 MG,TP 10,cGMP,TP10,inhibit,TP-10,disorder,Inhibitor,cAMP,reactive oxygen,Phosphodiesterase (PDE),pCREB-LI
[EINECS(EC#)]

604-604-1
[Molecular Formula]

C26H19F3N4O
[MOL File]

898563-00-3.mol
[Molecular Weight]

460.45
Chemical PropertiesBack Directory
[Boiling point ]

564.4±50.0 °C(Predicted)
[density ]

1.30±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 100 mg/mL (217.18 mM);Water : < 0.1 mg/mL (insoluble)
[form ]

Solid
[pka]

4.08±0.10(Predicted)
[color ]

Light yellow to brown
Hazard InformationBack Directory
[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]

[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

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