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VU0424238

Names

[ CAS No. ]:
1396337-04-4

[ Name ]:
VU0424238

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H12FN5O2

[ Molecular Weight ]:
325.30

[ Exact Mass ]:
325.09800

[ PSA ]:
89.89000

[ LogP ]:
2.83170

[ Storage condition ]:
2-8℃

Related Compounds