PDE2/PDE10-IN-1 is a phosphodiesterase 2 ( PDE2 ) and PDE10 inhibitor with IC 50 s of 29 and 480 nM, respectively. In Vitro PDE2/PDE10-IN-1 (Compound 6) inhibits PDE2 and PDE10, respectively, with an IC 50 value of 29 and 480 nM. PDE2/PDE10-IN-1 also inhibits PDE11A and PDE4D with IC 50 s of 6920 nM and 5890 nM, respectively. In addition PDE2/PDE10-IN-1 does not show significant inhibition of a panel of CYP450 enzymes (CYP1A2, 2C9, 2D6, 2C19, and 3A4). PDE2/PDE10-IN-1 is also inactive up to a concentration of 125 μg/mL in a bacterial mutagenicity assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 (t 1/2 =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 (t 1/2 =2.36 h), resulting in good bioavailability and a maximum plasma concentration (C max ) 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 ED 50 of 21 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:hPDE2A 29 nM (IC 50 ) rPDE10A 480 nM (IC 50 ) hPDE4D 5890 nM (IC 50 ) hPDE11A 6920 nM (IC 50 )
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PDE2/PDE10-IN-1
CAS number：1426833-08-0 molecular formula：C15H10ClN5
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1426833-08-0 | molecular formula | C15H10ClN5 |
| molecular weight | 295.73 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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