VU 0364439

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM. IC50 Value: 19.8 nM (EC50) Target: mGluR in vitro: in vivo: VU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining) .

Product Specifications

CAS Number

[1246086-78-1]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/VU-0364439.html

Purity

99.42

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=NC=CC=C1)NC2=CC=C(S(=O)(NC3=CC=CC=C3Cl)=O)C(Cl)=C2

Molecular Formula

C18H13Cl2N3O3S

Molecular Weight

422.29

Precautions

H315, H319, H335

References & Citations

[1]Hong, Sang-Phyo; Liu, Kevin G.; Ma, Gil et al. Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators. Journal of Medicinal Chemistry (2011), 54 (14), 5070-5081.|[2]Engers, Darren W.; Gentry, Patrick R.; Williams, Richard et al. Synthesis and SAR of novel 4- (phenylsulfamoyl) phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS) . Bioorganic & Medicinal Chemistry Letters (2010), 20 (17), 5175-5178.|[3]AJ Robichaud et al. Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics. ACS Chem. Neurosci. 2011, 2 (8), 433-449.