VU0477573

Modify Date: 2024-08-17 08:36:35

VU0477573 Structure
VU0477573 structure
Common Name VU0477573
CAS Number 1946021-40-4 Molecular Weight 296.339
Density 1.2±0.1 g/cm3 Boiling Point 472.3±40.0 °C at 760 mmHg
Molecular Formula C18H17FN2O Melting Point N/A
MSDS N/A Flash Point 239.4±27.3 °C

 Use of VU0477573


A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM; shows no activity against the other mGlu receptor subtypes (>10 uM); exhibits full occupancy of the MPEP site, does not completely inhibit maximal effects of mGlu5 agonists on intracellular calcium mobilization, inositol phosphate (IP) accumulation, or inhibition of synaptic transmission at the hippocampal Schaffer collateral-CA1 synapse; acts as a full NAM when measuring effects on mGlu5-mediated ERK1/2 phosphorylation; shows robust efficacy, comparable to the mGlu5 NAM MTEP, in models of anxiolytic activity.

 Names

Name N,N-Diethyl-5-[(3-fluorophenyl)ethynyl]-2-pyridinecarboxamide
Synonym More Synonyms

 VU0477573 Biological Activity

Description A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM; shows no activity against the other mGlu receptor subtypes (>10 uM); exhibits full occupancy of the MPEP site, does not completely inhibit maximal effects of mGlu5 agonists on intracellular calcium mobilization, inositol phosphate (IP) accumulation, or inhibition of synaptic transmission at the hippocampal Schaffer collateral-CA1 synapse; acts as a full NAM when measuring effects on mGlu5-mediated ERK1/2 phosphorylation; shows robust efficacy, comparable to the mGlu5 NAM MTEP, in models of anxiolytic activity.
References References 1. Nickols HH, et al. J Pharmacol Exp Ther. 2016 Jan;356(1):123-36. View Related Products by Target mGluR

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 472.3±40.0 °C at 760 mmHg
Molecular Formula C18H17FN2O
Molecular Weight 296.339
Flash Point 239.4±27.3 °C
Exact Mass 296.132477
LogP 3.23
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.589

 Synonyms

MFCD30146434
2-Pyridinecarboxamide, N,N-diethyl-5-[2-(3-fluorophenyl)ethynyl]-
N,N-Diethyl-5-[(3-fluorophenyl)ethynyl]-2-pyridinecarboxamide