PDE2/PDE10-IN-1 - 10mM in DMSO , CAS No.1426833-08-0

CAS: 1426833-08-0 Cat. No.: P654792 Summenformel: C₁₅H₁₀ClN₅ Molekulargewicht: 295.73

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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.

IC50& Target:hPDE2A 29 nM (IC 50 ) rPDE10A 480 nM (IC 50 ) hPDE4D 5890 nM (IC 50 ) hPDE11A 6920 nM (IC 50 )

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

PDE2/PDE10-IN-1 is a phosphodiesterase 2 ( PDE2 ) and PDE10 inhibitor with IC 50 s of 29 and 480 nM, respectively.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Namen und Kennungen

• Molekulargewicht: 295.73

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1426833-08-0, the molecular formula is C15H10ClN5, and the molecular weight is 295.73 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.