名称 | SCH-336 |
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. |
体外活性 | 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]. |
体内活性 | 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]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 90.0 mg/mL (48.6 mM)
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关键字 | SCH-336 | SCH-225336 |
相关产品 | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | CB1 inverse agonist 1 | Pregnenolone acetate | CB1 antagonist 2 | OMDM-5 | CB2 receptor agonist 2 | AM-1235 | 2,3-Butanediol | Drinabant | AM281 |
相关库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 已知活性化合物库 | GPCR靶点分子库 |