Dipraglurant

Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo[1][2]. Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[872363-17-2]

Product Name Alternative

ADX48621

UNSPSC

12352005

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Dipraglurant.html

Concentration

10mM

Purity

99.97

Solubility

DMSO : ≥ 40 mg/mL

Smiles

FC1=CN2C(C=C1)=NC(CCC#CC3=NC=CC=C3)=C2

Molecular Formula

C16H12FN3

Molecular Weight

265.29

References & Citations

[1]Bezard E, et, al. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov Disord. 2014 Jul;29 (8) :1074-9.|[2]Sciamanna G, et, al. Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia. Neuropharmacology. 2014 Oct;85:440-50.|[3]The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12