Identification | Back Directory | [Name]
PDE2/PDE10-IN-1 | [CAS]
1426833-08-0 | [Synonyms]
PDE2/PDE10-IN-1 Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine, 1-(2-chlorophenyl)-4-methyl- | [Molecular Formula]
C15H10ClN5 | [MDL Number]
MFCD31619317 | [MOL File]
1426833-08-0.mol | [Molecular Weight]
295.73 |
Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
1.72±0.50(Predicted) | [color ]
Off-white to brown |
Hazard Information | Back Directory | [Uses]
PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively. | [in vivo]
The PK properties of PDE2/PDE10-IN-1 are studied in rats after 2.5 mg/kg i.v. and 10 mg/kg p.o. administration. After i.v. administration, a rapid clearance is observed (t1/2=0.47 h), which is not expected based on the in vitro metabolic stability in rat liver microsomes (rLMs). Interestingly, PDE2/PDE10-IN-1 shows much slower clearance after p.o. administration (t1/2=2.36 h), resulting in good bioavailability and a maximum plasma concentration (Cmax) of 997 ng/mL. PDE2/PDE10-IN-1 is assessed for its potential to cross the blood–brain barrier in rats after 10 mg/kg s.c. administration. PDE2/PDE10-IN-1 shows good formulatability with 10 to 20% HPβCD at pH>3.5. The brain concentration for PDE2/PDE10-IN-1 after 1 h administration is in the range of 370-895 ng/g with high brain free fractions and brain/plasma ratios. More specifically, PDE2/PDE10-IN-1, which is orally bioavailable, occupies PDE2 with an ED50 of 21 mg/kg[1]. | [IC 50]
hPDE2A: 29 nM (IC50); rPDE10A: 480 nM (IC50); hPDE4D: 5890 nM (IC50); hPDE11A: 6920 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Rombouts FJ, et al. Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors. ACS Med Chem Lett. 2015 Jan 15;6(3):282-6. DOI:10.1021/ml500463t |
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