VU0364439

Cas No.:	1246086-78-1
Synonyms:	VU0 364439; VU-0364439
SMILES:	C1=CC=C(C(=C1)NS(=O)(=O)C2=C(C=C(C=C2)NC(=O)C3=CC=CC=N3)Cl)Cl
Formula:	C18H13Cl2N3O3S
M.Wt:	422.29
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
Target:	IC50 Value: 19.8 nM(EC50) Target: mGluR
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).
References:	[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 Chem [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.