VU0483605

Modify Date: 2024-01-05 12:35:43

VU0483605 Structure
VU0483605 structure
Common Name VU0483605
CAS Number 1623101-11-0 Molecular Weight 446.67
Density 1.6±0.1 g/cm3 Boiling Point N/A
Molecular Formula C20H10Cl3N3O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of VU0483605


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].

 Names

Name 2-Chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)phenyl]nicotinamide
Synonym More Synonyms

 VU0483605 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
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

 Synonyms

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]-
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