Auglurant (VU0424238) 是一种新型的有选择性的 mGlu5 拮抗剂，抑制大鼠 mGlu5 的 IC50 值为 11 nM，人 mGlu5 的 IC50 值为 14 nM。Auglurant (VU0424238) 可渗透通过神经系统。
货号:ajcx39484
CAS:1396337-04-4
分子式:C16H12FN5O2
分子量：325.3
溶解度:DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration[1].

Auglurant (VU0424238) with an IC50 value of 14 nM in HEK293A cells. It also binding a known allosteric site with K i value of 4.4 nM in HEK293A cells.

Auglurant (VU0424238) had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monkeys and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons[1].

[1]. Felts AS, et al. Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085.