1396337-04-4

1396337-04-4 structure

Name: VU0424238
Chemical Name: N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide
CAS Number: 1396337-04-4
Molecular Formula: C₁₆H₁₂FN₅O₂
Molecular Weight: 325.30
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2018-03-10 16:31:45
Modify Date: 2024-01-09 12:33:30
VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration[1].

Name	N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide

Description	VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
In Vitro	VU0424238 with an IC50 value of 14 nM in HEK293A cells. It also binding a known allosteric site with K i value of 4.4 nM in HEK293A cells.
In Vivo	VU0424238 had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monkeys and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons[1].
References	[1]. Felts AS, et al. Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085.