化合物 SR144528
| 中文名称 | 化合物 SR144528 |
|---|---|
| 中文同义词 | 化合物 T16928;5-(4-氯-3-甲基苯基)-1-(4-甲基苄基)-N-((1S,2S,4R)-1,3,3-三甲基双环[2.2.1]庚烷-2-基)-1H-吡唑-3-甲酰胺;化合物 SR144528;化合物SR144528,10 MM DMSO 溶液;5-(4-氯-3-甲基苯基)-1-[(4-甲基苯基)甲基]-N-[(1S,2S,4R)-1,3,3-三甲基双环[2.2.1]HEPT-2-YL]-1H-吡唑-3-甲酰胺 |
| 英文名称 | SR 144528 |
| 英文同义词 | SR 144528;5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide;1H-Pyrazole-3-carboxamide, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-;SR-144528,SR144528;5-(4-Chloro-3-methylphenyl)-1-(4-methylbenzyl)-N-((1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl)-1H-pyrazole-3-carboxamide;5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl]-1H-pyrazole-3-carboxamide;SR144528, 10 mM in DMSO |
| CAS号 | 192703-06-3 |
| 分子式 | C29H34ClN3O |
| 分子量 | 476.05 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 192703-06-3.mol |
| 结构式 |  |
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 |
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.
安全信息
| WGK Germany | WGK 3 |
|---|---|
| RTECS号 | UQ6276700 |
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-13439 | 化合物 SR144528 SR144528 | 192703-06-3 | 1 mg | 396元 |
| 2026/06/05 | HY-13439 | 192703-06-3 SR144528 | 192703-06-3 | 5mg | 990元 |