首页 GPCR/G Protein Histamine Receptor GSK189254A
GSK189254A
编号 TQ0066     别名: GSK189254
CAS 720690-73-3     分子式 C21H25N3O2     分子量 351.44
靶点:
GSK189254A (GSK189254) is a new, potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).
选择批次  
纯度 98.00%
规格 库存 单价 数量
10 mg 待询 2400.00
25 mg 待询 5000.00
50 mg 待询 7200.00
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生物活性

产品描述

GSK189254A (GSK189254) is a new, 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

体外活性

GSK189254 has a high affinity for both recombinant H3 receptors expressed in HEK-293-MSR-II cells and native H3 receptors expressed in the cerebral cortex of several species. GSK189254 generally exhibits a higher affinity for human and pig H3 receptors compared with mouse, rat, and dog H3 receptors. GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer's disease and other cognitive disorders [1].

体内活性

In Ox+/+ and Ox−/− mice, acute administration of GSK189254 increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox−/− mice [2]. GSK189254 (0.3-3 mg/kg p.o.) increases the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improves the performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift [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].

化学信息

分子量

351.44

分子式

C21H25N3O2

CAS

720690-73-3

溶解度

DMSO: 24 mg/mL (68.29 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

冷藏

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.845 ml 14.227 ml 28.454 ml
5 mM 0.569 ml 2.845 ml 5.691 ml
10 mM 0.285 ml 1.423 ml 2.845 ml
50 mM 0.057 ml 0.285 ml 0.569 ml
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