规格

价格

库存

数量

1 mg

¥ 493

现货

5 mg

¥ 828

现货

10 mg

¥ 1,230

现货

25 mg

¥ 2,270

现货

50 mg

¥ 3,390

现货

100 mg

¥ 4,930

现货

200 mg

¥ 6,880

现货

1 mL x 10 mM (in DMSO)

¥ 638

现货

生物活性

产品描述	GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).
靶点活性	H3 receptor (human):9.59-9.90 (pKi), H3 receptor (mouse):8.51-9.17 (pKi)
体外活性	GSK189254 对于在HEK-293-MSR-II细胞中表达的重组H3受体以及多种物种大脑皮层中表达的天然H3受体均具有高亲和力。GSK189254 通常对人类和猪的H3受体展现出更高的亲和力，相比之下，与小鼠、大鼠和狗的H3受体的亲和力较低。GSK189254 可能对阿尔茨海默病和其他认知障碍的症状性治疗具有潜在的治疗价值[1]。
体内活性	在Ox+/+和Ox/小鼠中，GSK189254的急性给药能够增加W，降低慢波睡眠和反常睡眠的程度，与modafinil相似，同时在Ox/小鼠中减少了发作的纳尔科病次数[2]。GSK189254（0.3-3 mg/kg p.o.）增加了前扣带皮质中乙酰胆碱、去甲肾上腺素和多巴胺的释放，以及在背侧海马中的乙酰胆碱释放。GSK189254显著提高了在多种认知范式中大鼠的表现，包括被动避免、水迷宫、物体识别和注意集合转移[1]。
动物实验	Pharmacokinetic studies with GSK189254 are conducted in conscious male Sprague-Dawley rats. Animals receive an intravenous infusion of GSK189254 (n=3) administered at a nominal dose level of 1 mg of free base/kg for 1 h via the femoral vein cannula (10 mL/h/kg). GSK189254 is dissolved in 0.9% (w/v) saline at a target concentration of 0.1 mg free base/mL and filtered with a 0.22-mm Millex-GV filter before administration. After an ish out of at least 2 days, the same rats received a single oral administration of GSK189254 by gastric gavage to achieve a target dose of 2 mg of free base/kg. GSK189254 is formulated in 1% (w/v) aqueous methylcellulose at a target concentration of 0.4 mg free base/mL [1]. The vehicle consists of 0.05 mL NaCl at 0.9% containing methylcellulose at 1%. GSK189254 is a dissolved in-vehicle solution. The effects of acute and repeat administration of GSK189254 on the sleep-wake cycle in wild-type (Ox+/+) and orexin knockout (Ox?/?) mice is investigated. GSK189254 (3 and 10 mg/kg, p.o.) is administered on the sleep-wake cycle in Ox+/+ and Ox?/? mice, dosed at 10 h. The oral administration dose of GSK189254 is 10 mg/kg [2].
别名	GSK189254

化学信息

分子量	351.44
分子式	C₂₁H₂₅N₃O₂
CAS No.	720690-73-3
Smiles	CNC(=O)c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1
密度	1.195 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

store at low temperature | 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

DMSO: 24 mg/mL (68.29 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.69 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8454 mL	14.2272 mL	28.4544 mL	142.2718 mL
5 mM	0.5691 mL	2.8454 mL	5.6909 mL	28.4544 mL
10 mM	0.2845 mL	1.4227 mL	2.8454 mL	14.2272 mL
20 mM	0.1423 mL	0.7114 mL	1.4227 mL	7.1136 mL
50 mM	0.0569 mL	0.2845 mL	0.5691 mL	2.8454 mL