SCH-336

SCH-336CAS号: 447459-51-0分子式: C23H25NO8S3分子量: 539.64描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
SCH-336 is a CB2 receptor agonist (Ki-1.8 nM, EC50-2 nM) with effective, selective, and oral activity. SCH-336 is also bioactive against CB1 receptor, and is 100 times more selective to CB2 receptor than CB1. SCH-336 reduced the binding of guanosine 5′ -3-o -(sulfur) triphosphate to the membrane containing hCB, inhibited BaF3/CB2 cell migration, inhibited leukocyte migration in mouse delayed hypersensitivity models, and inhibited antigen-induced pulmonary eosinophilia in mouse allergy models.
纯度
95%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:90.0 mg/mL (48.6 mM)
生物活性
靶点
human CB1:200nM(EC50), human CB2:2nM(EC50), BaF3/CB2:34nM
In vitro(体外研究)
SCH 336 (also known as Sch.336) exhibits competitive binding with [3H]CP55,940 to human CB2 receptors on Sf9 cell membranes, with a Ki value of 1.8 nM. It reduces GTPγS binding on membranes containing human CB2 receptors, with an EC50 of 2 nM. However, its potency decreases on membranes containing CB1 receptors, with an EC50 of 200 nM [1]. Moreover, SCH 336 inhibits the migration of BaF3/CB2 cells towards 100 nM 2-AG, with an IC50 of 34 nM [1].
In vivo(体内研究)
In in vivo studies, when administered intraperitoneally (i.p.) at doses of 0.02-2.0 mg/kg, SCH 336 significantly inhibits leukocyte migration [1].