513050

PDE10A Inhibitor, Cpd15

• Synonym(s): PDE10A Inhibitor, Cpd15, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol, Phosphodiesterase 10A Inhibitor
• Empirical Formula (Hill Notation): C₁₈H₁₆ClN₅O
• Molecular Weight: 353.81
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: ≤5 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C

Description

General description

A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (K_i≤5 nM against human PDE10A-catalyzed cAMP hydrolysis), while exhibiting >500-fold selectivity over other human PDEs 1-11 and much reduced or little activity against CYP3A4 (IC₅₀ = 7.9 and >20 µM, respectively, with or without preincubation) as well as a panel of 23 kinases (IC₅₀ >30 µM). Reported to be orally available in monkey (AUC_{0-6 h} = 11,496 nM·h, T_1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC_{0-6 h}475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo.

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett.22, 1335.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable