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。
| 生物活性 | AM281 is a selectiveCB1receptorantagonist with anIC50of 9.91 nM. AM281 inhibitsCB2receptor with an IC50of 13000 nM[1]. |
| IC50& Target[1] | CB1 9.91 nM (IC50) | CB2 13000 nM (IC50) |
|
体外研究
(In Vitro) | 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[2].
|
体内研究
(In Vivo) | 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[3].
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[3].
| Animal Model: | Male NMRI mice with the weight of 25-30 g[3] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 7.14 mg/mL(12.81 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.7947 mL | 8.9733 mL | 17.9466 mL | | 5 mM | 0.3589 mL | 1.7947 mL | 3.5893 mL | | 10 mM | 0.1795 mL | 0.8973 mL | 1.7947 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 0.71 mg/mL (1.27 mM); Clear solution
此方案可获得 ≥ 0.71 mg/mL (1.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
m.cnreagent.com