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ADX-47273

Catalog No.
B1632
mGluR5 receptor positive allosteric modulator, potent and selective
Grouped product items
SizePriceStock Qty
5mg
$72.00
Ship with 10-15 days
10mg
$115.00
Ship with 10-15 days
50mg
$431.00
Ship with 10-15 days
100mg
$672.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

ADX-47273 is a potent and selective mGluR5 receptor PAM (positive allosteric modulator), EC50 = 0.17 μm, with no effect on other mGluR subtypes. [1]

The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. It plays a critical role in regulating synaptic plasticity and neural network activity.

In HEK-293 cell expressing rat mGlu5, ADX-showed 9-fold higher response (EC50 = 0.17 μm) to threshold concentration of glutamate (50 nM) in the fluorometric Ca2+ assays, it also shifted mGlu5 receptor glutamate response curve to the left. [1]

In vivo, ADX47273 increased ERK (extracellular signal-regulated kinase) and CREB (cAMP-responsive element-binding protein) phosphorylation in rat hippocampus and prefrontal cortex. In rat and mouse models that sensitive to antipsychotic treatment, ADX47273 decreased rat conditioned avoidance responding (minimal effective dose = 30 mg/kg i.p.) and reduced mouse ampomorphine-activated climbing (minimal effective dose = 100 mg/kg i.p.) [1]

Reference:
[1] Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, Marquis KL.  ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and precognitive activities.  J Pharmacol Exp Ther. 2008 Dec;327(3):827-39.

Chemical Properties

StorageStore at -20°C
M.Wt369.36
Cas No.851881-60-2
FormulaC20H17F2N3O2
SolubilitySoluble in DMSO
Chemical Name(4-fluorophenyl)-[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl]methanone
SDFDownload SDF
Canonical SMILESC1CC(CN(C1)C(=O)C2=CC=C(C=C2)F)C3=NC(=NO3)C4=CC=C(C=C4)F
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

ADX-47273