Quality Level
InChI
1S/C11H11ClN4O2/c1-16-6-9(17)14-10(16)15-11(18)13-8-4-2-3-7(12)5-8/h2-5H,6H2,1H3,(H2,13,14,15,17,18)
InChI key
DWPQODZAOSWNHB-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
potency
87 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
General description
A potent negative allosteric modulator highly selective for mGluR5 (IC50 = 87 nM; Kd = 54 nM and 31 nM at recombinant mGlu5 receptors of rat and human, respectively). Biologically active admitted orally or systematically. Frequently used for assessing the functional roles of mGlu5 receptors in a variety of brain functions (i.e. learning and memory, circadian rhythms, reward and decision making, and locomotion) and disorders (i.e. addition, depression, seizures, anxiety disorder, Parkinson′s disease, Alzheimer′s disease, and Down syndrome). A leading therapeutic candidate for treatment of fragile X syndrome.
Biochem/physiol Actions
Primary Target
mGlu₅ receptors
mGlu₅ receptors
Target Ki: 54 nM and 31 nM at recombinant mGlu₅ receptors of rat and human, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Porter, R., et al. 2005. J. Pharmacol. Exp. Ther.315, 711.
Jacob, W., et al. 2009. Neuropharmacology57, 97.
Berry-Kravis, E., et al. 2009. J. Medical Genetics.46, 266.
Watterson, R., et al. 2012. Psychopharmacol.2012, 1.
Simonyi, A., et al. 2010. Eur. J. Pharmacol.639, 17.
Westmark, J., et al. 2010. J. Alzheimer′s Disease20, 1009.
Jacob, W., et al. 2009. Neuropharmacology57, 97.
Berry-Kravis, E., et al. 2009. J. Medical Genetics.46, 266.
Watterson, R., et al. 2012. Psychopharmacol.2012, 1.
Simonyi, A., et al. 2010. Eur. J. Pharmacol.639, 17.
Westmark, J., et al. 2010. J. Alzheimer′s Disease20, 1009.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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