VU 0424465

Modify Date: 2024-04-05 16:48:00

VU 0424465 Structure
VU 0424465 structure
Common Name VU 0424465
CAS Number 1428630-85-6 Molecular Weight 326.36
Density 1.2±0.1 g/cm3 Boiling Point 533.8±50.0 °C at 760 mmHg
Molecular Formula C19H19FN2O2 Melting Point N/A
MSDS N/A Flash Point 276.7±30.1 °C

 Use of VU 0424465


VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons[1][2].

 Names

Name VU0424465
Synonym More Synonyms

 VU 0424465 Biological Activity

Description VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons[1][2].
Related Catalog
Target

mGlu5

In Vitro VU0424465 exhibits robust agonist activity and induces calcium mobilization in the absence of glutamate (EC50 = 171 ± 15 nM, maximum efficacy 65% compared to glutamate)[2]. VU0424465 potentiates glutamate-induced calcium mobilization, with EC50 of 1.5 ± 0.8 nM[2]. VU0424465 shows significant bias away from iCa2+ mobilization and toward IP1 accumulation (110-fold) and ERK1/2 phosphorylation (9-fold) in HEK293A-mGlu5-low cells[1].
References

[1]. Sengmany K, et al. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017;115:60-72.

[2]. Rook JM, Noetzel MJ, Pouliot WA, et al. Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol Psychiatry. 2013;73(6):501-509.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 533.8±50.0 °C at 760 mmHg
Molecular Formula C19H19FN2O2
Molecular Weight 326.36
Flash Point 276.7±30.1 °C
Exact Mass 326.143066
LogP 2.95
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.594

 Synonyms

5-[(3-Fluorophenyl)ethynyl]-N-[(2R)-3-hydroxy-3-methyl-2-butanyl]-2-pyridinecarboxamide
2-Pyridinecarboxamide, 5-[2-(3-fluorophenyl)ethynyl]-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-
VU0424465
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