VU0424238

Modify Date: 2024-01-09 12:33:30

VU0424238 Structure
VU0424238 structure
Common Name VU0424238
CAS Number 1396337-04-4 Molecular Weight 325.30
Density N/A Boiling Point N/A
Molecular Formula C16H12FN5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of VU0424238


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].

 Names

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

 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
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℃