1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺
| 中文名称 | 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺 |
|---|---|
| 中文同义词 | 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺;1-(2,4-二氯苯)-5-(4-碘苯基)-4-甲基-N-4-吗啉基-1H-吡唑-3-甲酰胺;化合物AM281;化合物AM281,10 MM DMSO 溶液 |
| 英文名称 | 1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE |
| 英文同义词 | AM-281 ,99%;1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE;AM 281;CS-1127;AM281;AM-281;1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide AM 281;1H-Pyrazole-3-carboxamide,1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-;1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide |
| CAS号 | 202463-68-1 |
| 分子式 | C21H19Cl2IN4O2 |
| 分子量 | 557.21 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;Inhibitors;Cannabinoid receptor;Cannabinoids. |
| Mol文件 | 202463-68-1.mol |
| 结构式 |  |
1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺 性质
| 密度 | 1.70±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：>6 mg/mL |
| 酸度系数(pKa) | 10.76±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| InChI | 1S/C21H19Cl2IN4O2/c1-13-19(21(29)26-27-8-10-30-11-9-27)25-28(18-7-4-15(22)12-17(18)23)20(13)14-2-5-16(24)6-3-14/h2-7,12H,8-11H2,1H3,(H,26,29) |
| InChIKey | AJFFBPZYXRNAIC-UHFFFAOYSA-N |
| SMILES | Cc1c(nn(-c2ccc(Cl)cc2Cl)c1-c3ccc(I)cc3)C(=O)NN4CCOCC4 |
|
CB1 9.91 nM (IC 50 ) |
CB2 13000 nM (IC 50 ) |
AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6.
Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281.
Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory.
| Animal Model: | Male NMRI mice with the weight of 25-30 g |
| Dosage: | 0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration) |
| Administration: | Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration) |
| Result: |
The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle.
Acute administration at a dose of 5 mg/kg, significantly augmented recognition index. |
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 25-36/37/38 |
| 安全说明 | 26-36/37/39-45 |
| 危险品运输编号 | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| 存储类别 | 6.1A - 可燃，急性毒性物质（类别1和类别2） 剧毒的危险物质 |
| 危险性类别 | 急性毒性 类别2 经口 眼部刺激 类别2 经皮刺激 类别2 特异性靶器官毒性-一次接触，类别3 |
| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-13505 | 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺 AM281 | 202463-68-1 | 1 mg | 838元 |
| 2025/12/22 | HY-13505 | 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-吗啉-1H-吡唑-3-甲酰胺 AM281 | 202463-68-1 | 5 mg | 2200元 |