VU0424238 - mGlu5 Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVU0424238Cat. No.: HY-16617CAS No.: 1396337-04-4分式: CHFNO分量: 325.3作靶点: mGluR作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 22.73 mg/mL (69.87 mM; Nee

2、d ultrasonic)H2O : 90% corn oilSolubility: 2.08 mg/mL (6.39 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 VU0424238种新型的有选择性的 mGlu5 拮抗剂，抑制 mGlu5 的 IC50 值为 11 nM， mGlu5 的 IC50值为 14 nM。VU0424238 可渗透通过神经系统 1。体外研究 VU0424238 with an IC50 value of 14 nM in HEK29

3、3A cells. It also binding a known allosteric site with K i valueof 4.4 nM in HEK293A cells.体内研究 VU0424238 had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy atan oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monke

4、ys anddemonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons 1.REFERENCES1. Felts AS, et al. Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel NegativeAllosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun22;60(12):5072-5085.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;F