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513050 PDE10A Inhibitor, Cpd15 - Calbiochem

PDE10A Inhibitor, Cpd15 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Phosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol

513050
  
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Přehled

Replacement Information

Tabulka spec. kláve

Empirical Formula
C₁₈H₁₆ClN₅O
Description
Overview

This product has been discontinued.



A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20 µM) or a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey and rat species and be efficacious in reversing NMDAR antagonist (+)-MK-801- (Cat. No. 475878) induced hyperactivity in a ratsl (MED = 10 mg/kg p.o.) in vivo.
Catalogue Number513050
Brand Family Calbiochem®
SynonymsPhosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol
References
ReferencesMcElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.
Product Information
FormOff-white powder
Hill FormulaC₁₈H₁₆ClN₅O
Chemical formulaC₁₈H₁₆ClN₅O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Target K<sub>i</sub>≤5 nM
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
513050 0

Documentation

PDE10A Inhibitor, Cpd15 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

PDE10A Inhibitor, Cpd15 - Calbiochem Certificates of Analysis

TitleLot Number
513050

References

Přehled odkazů
McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision11-March-2013 JSW
SynonymsPhosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol
DescriptionA cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤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 (AUC0-6 h = 11,496 nM·h, T1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC0-6 h475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₈H₁₆ClN₅O
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMcElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335.