1623101-11-0

1623101-11-0 structure

Name: VU0483605
Chemical Name: 2-Chloro-N-[3-chloro-4-(4-chloro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)phenyl]nicotinamide
CAS Number: 1623101-11-0
Molecular Formula: C₂₀H₁₀Cl₃N₃O₃
Molecular Weight: 446.67
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2016-05-05 19:37:08
Modify Date: 2024-01-05 12:35:43
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].

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

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.