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
- CAS号:202463-68-1
- 英文名:1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-4-MORPHOLINYL-1H-PYRAZOLE-3-CARBOXAMIDE
- 中文名: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
- CBNumber:CB9297436
- 分子式:C21H19Cl2IN4O2
- 分子量:557.21
- MOL File:202463-68-1.mol
- 密度 :1.70±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: >6 mg/mL
- 形态 :solid
- 酸度系数(pKa) :10.76±0.20(Predicted)
- 颜色 :white
- 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
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、用途与生产工艺
- 生物活性 AM281 是一种选择性 CB1 受体拮抗剂，IC50 为 9.91 nM。AM281 抑制 CB2 受体，IC50 为 13000 nM。
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靶点
CB1
9.91 nM (IC 50 )
CB2
13000 nM (IC 50 )
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体外研究
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.
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体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-13505
- 产品名称：AM281
- CAS编号：
- 包装：1 mg
- 价格：838元
- 更新日期：2024/11/08
- 产品编号：HY-13505
- 产品名称：AM281
- CAS编号：
- 包装：5 mg
- 价格：2200元
- 公司名称：MOLEKULA
- 联系电话：--
- 电子邮件：kevinbanks@molekula.com
- 国家：英国
- 产品数：6140
- 优势度：66
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
