Shanghai Nianxing Industrial Co., Ltd
China
Product Name: PDE2/PDE10-IN-1
Price: Check
Purity: 99.0%
Stocking Period: 10 Day
Contact: Yang
Email: sales@echemcloud.com

1426833-08-0

1426833-08-0 structure

1426833-08-0 structure

Name: PDE2/PDE10-IN-1
Chemical Name: PDE2/PDE10-IN-1
CAS Number: 1426833-08-0
Molecular Formula: C₁₅H₁₀ClN₅
Molecular Weight: 295.73
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2018-05-30 04:15:40
Modify Date: 2025-08-27 08:03:52
PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.

Name	PDE2/PDE10-IN-1

Description	PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Neurological Disease
Target	hPDE2A:29 nM (IC50) rPDE10A:480 nM (IC50) hPDE4D:5890 nM (IC50) hPDE11A:6920 nM (IC50)
In Vitro	PDE2/PDE10-IN-1 (Compound 6) inhibits PDE2 and PDE10, respectively, with an IC50 value of 29 and 480 nM. PDE2/PDE10-IN-1 also inhibits PDE11A and PDE4D with IC50s 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[1].
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].
Animal Admin	Rats[1] Male Sprague-Dawley rats are fed with PDE2/PDE10-IN-1 (i.v., 2.5 mg/kg; p.o., 10 mg/kg). After administration, the clearance is observed.
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.

Molecular Formula	C₁₅H₁₀ClN₅
Molecular Weight	295.73

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.