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About This Item
Empirical Formula (Hill Notation):
C23H16N4O
CAS Number:
Molecular Weight:
364.40
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C23H16N4O/c24-16-17-8-7-11-19(14-17)23(28)25-22-15-21(18-9-3-1-4-10-18)26-27(22)20-12-5-2-6-13-20/h1-15H,(H,25,28)
InChI key
BKUIZWILNWHFHD-UHFFFAOYSA-N
General description
A pyrazole amide compound that crosses the blood-brain barrier and acts as a potent, selective, reversible, positive allosteric modulator for metabotropic glutamate receptor subtype 5 (mGluR5). Also exerts anti-psychotic-like effects. Reported to potentiate the response to glutamate (~300 nM) in CHO-mGluR5 cells (EC50 = 10 nM for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation) and reverse amphetamine-induced disruption of pre-pulse inhibition (PPI) in rats. Specificity was determined using a panel of kinases and receptors. Does not potentiate the activity of other glutamate receptors.
Biochem/physiol Actions
Cell permeable: no
EC50 = 10 nM in potentiating the response to glutamate (~300 nM) in CHO-mGluR5 cells for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation
Primary Target
Metabotropic glutamate receptor subtype 5 (mGluR5)
Metabotropic glutamate receptor subtype 5 (mGluR5)
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Kinney, G.G., et al. 2005. J. Pharmacol. Exp. Ther.313, 199.
Lindsley, C.W., et al. 2004. J. Med. Chem.47, 5825.
Lindsley, C.W., et al. 2004. J. Med. Chem.47, 5825.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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