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VU0483605

Catalog No.
C5611
elective positive allosteric modulator (PAM) of mGluR1
Grouped product items
SizePriceStock Qty
5mg
$132.00
Ship with 5-10 days
10mg
$228.00
Ship with 5-10 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

VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1 [1].

The metabotropic glutamate receptors (mGluRs), members of G-protein-coupled receptors, have been involved in a variety of functions in the central and peripheral nervous systems, such as learning, memory, anxiety, and the perception of pain. The mGluRs exist in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Mice deficient in mGluR1 showed severe motor coordination and spatial learning deficient [2].

VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1. VU0483605 displayed EC50 values of 0.39 and 0.36 μM at human and rat mGluR1 receptors, respectively. VU0483605 showed no activity against mGlu4 PAM with the EC50 of >10 μM. VU0483605 potentiated the response to glutamate in cells stably expressing mGlu1 and partially restored the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia [1].

References:
[1] Cho H P, Garcia-Barrantes P M, Brogan J T, et al.  Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics[J]. ACS chemical biology, 2014, 9(10): 2334-2346.
[2] Conquet F, Bashir Z I, Davies C H, et al.  Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1[J]. Nature, 1994, 372(6503): 237.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt446.7
Cas No.1623101-11-0
FormulaC20H10Cl3N3O3
Solubility≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Name3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
SDFDownload SDF
Canonical SMILESO=C1N(C2=CC=C(NC(C3=C(Cl)C=CC=N3)=O)C=C2Cl)C(C4=CC=CC(Cl)=C41)=O
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

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Chemical structure

VU0483605