<Suppliers Price>

VU0483605

Names

[ CAS No. ]:
1623101-11-0

[ Name ]:
VU0483605

[Synonym ]:
vu0483605
3-Chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
2-Pyridinecarboxamide, 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-

Biological Activity

[Description]:

VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> mGluR

[Target]

Human mGluR1:390 nM (EC50)

rat mGluR1:356 nM (EC50)

Human mGlu4:>10 μM (EC50)


[In Vitro]

VU0483605 proves superior with excellent mGlu1 PAM activity at both human (EC50 = 390 nM) and rat (EC50 = 356 nM, pEC50 = 6.45 ± 0.11, 113 ± 5% Glu Max) and no activity as an mGlu4 PAM (EC50 >10 μM)[1].

[References]

[1]. Cho HP, Garcia-Barrantes PM, Brogan JT, et al. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. ACS Chem Biol. 2014;9(10):2334-2346.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C20H10Cl3N3O3

[ Molecular Weight ]:
446.67

[ Exact Mass ]:
444.978760

[ LogP ]:
3.87

[ Index of Refraction ]:
1.728

[ Storage condition ]:
2-8°C

Related Compounds