1276617-62-9

1276617-62-9 structure

Name: VU 0409106
Chemical Name: 3-Fluoro-N-(4-methyl-1,3-thiazol-2-yl)-5-(5-pyrimidinyloxy)benzamide
CAS Number: 1276617-62-9
Molecular Formula: C₁₅H₁₁FN₄O₂S
Molecular Weight: 330.337
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2021-01-09 11:39:20
Modify Date: 2024-01-11 17:59:42
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB)[1][2].

Name	3-Fluoro-N-(4-methyl-1,3-thiazol-2-yl)-5-(5-pyrimidinyloxy)benzamide
Synonyms	Benzamide, 3-fluoro-N-(4-methyl-2-thiazolyl)-5-(5-pyrimidinyloxy)- MFCD29081178 3-Fluoro-N-(4-methyl-1,3-thiazol-2-yl)-5-(5-pyrimidinyloxy)benzamide

Description	VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB)[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	mGlu5:24 nM (IC50)
In Vivo	VU0409106 (10 mg/kg; i.p.; once) penetrates the blood-brain barrier (BBB) and demonstrates good brain to plasma ratio that near unity[1]. Animal Model: CD-1 mice[1] Dosage: 10 mg/kg (10% Tween 80 formulation) Administration: Intraperitoneal injection. Result: 1.19Pharmacokinetic Parameters of VU0409106 in CD-1 mice[1]. IP (10 mg/kg) Plasma Tmax (h) 0.25 Plasma Cmax (ng/mL) 1450 Brain Tmax (h) 0.25 Brain Cmax (ng/mL) 1350 AUCplasma (ng/mL•h) 702 AUCbrain (ng/mL•h) 696 B/P ratio 0.99
References	[1]. Felts AS, et al. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. [2]. Morrison RD, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metab Dispos. 2012 Sep;40(9):1834-45.