化合物 SR144528
化合物 SR144528 性质
| 沸点 | 627.7±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 溶于 DMSO（高达 20 mg/ml，加热）。 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 11.52±0.60(Predicted) |
| 颜色 | 白色至米色 |
| 稳定性 | 可在-20°C下的DMSO中的溶液储存长达3个月。 |
| InChIKey | SUGVYNSRNKFXQM-XRHWURSXSA-N |
| SMILES | N1(CC2=CC=C(C)C=C2)C(C2=CC=C(Cl)C(C)=C2)=CC(C(N[C@@H]2C(C)(C)[C@@]3([H])C[C@]2(C)CC3)=O)=N1 |
化合物 SR144528 用途与合成方法
Ki: 0.6 nM (CB2 receptor)
SR144528 is a potent and selective CB2 receptor antagonist with a K i of 0.6 nM. SR144528 alone is able to stimulate in a concentration-dependent manner (EC 50 =26±6 nM, two experiments) the forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells with a maximum effect at 1 μM (4-fold stimulation) whereas at this concentration it has no significant effect on CHO-CB1 cells (15% inhibition). Raw 264.7 macrophages supplemented with SR144528 display reduced caspase-3 activity. SR144528 inhibits microsomal acyl-coenzymeA:cholesterol acyltransferase (ACAT) activity in a concentration-dependent manner with an IC 50 value of 3.6±1.1 μM. At 10 μM, SR144528 inhibits ACAT activities ~68%.
No effect on the binding of [ 3 H]-CP 55,940 to its specific sites in the brain is observed after either oral (up to 10 mg/kg) or i.c.v. (10 μg/animal) administration of SR144528 in mice. The occupancy by SR144528 of the spleen cannabinoid receptor is time-dependent and significant for at least 18 hours after oral administration at 3 mg/kg. SR144528 does not induce any significant effect on gastrointestinal (GI) motility when given alone. SR144528 does not block but enhances delayedgastric emptying.
化合物 SR144528 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-13439 | 化合物 SR144528 | 192703-06-3 | 1 mg | 396 |
| 2025-12-22 | HY-13439 | 192703-06-3 | 192703-06-3 | 5mg | 990 |
