GAT564 (Compound 15d) 是大麻素 1 受体 (CB1R) 的有效变构调节剂,对 cAMP 和β-arrestin2 的EC50s 分别为 87 和 320 nM。GAT564 显着促进正构配体与 hCB1R 的结合。GAT564 是一种有效的外用药剂,可显着降低眼压正常的青光眼小鼠模型中的眼内压 (IOP)。
产品描述
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor ( CB1R ) with EC 50 s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma [1].
分子式
C20H16N2O2S
分子量
348.42
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years