规格

价格

库存

数量

1 mg

¥ 197

现货

5 mg

¥ 395

现货

10 mg

¥ 690

现货

25 mg

¥ 1,330

现货

50 mg

¥ 2,370

现货

100 mg

¥ 3,520

现货

500 mg

¥ 7,630

待询

1 mL x 10 mM (in DMSO)

¥ 485

现货

生物活性

产品描述	AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).
靶点活性	GPR55:39 nM, CB1:8 nM
体外活性	AM251对逃避任务中的记忆巩固有抑制作用.与对照组相比,AM251使测试的潜伏期明显减少,但在开放的户外适应性任务中却未发现差异,包括交叉口的数量.在相关的恐惧记忆测试中,经AM251（4.0/8.0 mg/kg）预处理的动物僵硬表现增强.AM251使大鼠每日摄食量持续减少.AM251会使大鼠出现挑食和与恶心相关的行为,但对摄食率无影响.
体内活性	通过变构性加速[3H]-箭毒蛙毒素A 20-α-苯甲酸盐:钠离子通道复合物的解离,AM251可抑制平衡结合。AM251使放射性配体的Kd增加2.3倍,而不影响Bmax。AM251可使藜芦定依赖性(河豚毒素抑制性) L-谷氨酸（IC50：8.5 μM）和GABA（IC50：9.2 μM）从突触体的释放减少。AM251使未刺激的和乙酰化LDL-刺激的Raw 264.7巨噬细胞减少,并减少CB2+/+和CB2 ?/?腹膜巨噬细胞中胆固醇酯的合成。
激酶实验	Macrophages are seeded (2×106/well) in 12-well culture plates. AM-251 or SR144528 are added from 4 mM stock solutions prepared in DMSO, 1h prior to the addition of 7-ketocholesterol (7KC) from a 2 mg/mL ethanol stock solution. Controls are adjusted to receive equivalent volumes of DMSO and ethanol. After 16 h, caspase-3 activity is determined. All treatments are done in triplicate and the data presented as the mean RFLU/mg protein±SD[3].

化学信息

分子量	555.24
分子式	C₂₂H₂₁Cl₂IN₄O
CAS No.	183232-66-8
Smiles	CC1=C(N(N=C1C(NN2CCCCC2)=O)C3=C(Cl)C=C(Cl)C=C3)C4=CC=C(I)C=C4
密度	1.65 g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: 13.9 mg/mL (25.03 mM), Sonication is recommended.

DMSO: 51.5 mg/mL (92.75 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.6 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8010 mL	9.0051 mL	18.0102 mL	90.0511 mL
5 mM	0.3602 mL	1.8010 mL	3.6020 mL	18.0102 mL
10 mM	0.1801 mL	0.9005 mL	1.8010 mL	9.0051 mL
20 mM	0.0901 mL	0.4503 mL	0.9005 mL	4.5026 mL