首页 GPCR/G Protein Histamine Receptor JNJ-5207852
JNJ-5207852
编号 T7413    
CAS 398473-34-2     分子式 C20H32N2O     分子量 316.48
靶点: rat H3R; human H3R;
JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.
选择批次  
规格 库存 单价 数量
2 mg 上海现货 698.00
5 mg 上海现货 997.00
10 mg 上海现货 1957.00
25 mg 上海现货 3527.00
50 mg 上海现货 6327.00
100 mg 上海现货 11217.00
1 mL * 10 mM (in DMSO) 上海现货 1087.00
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生物活性

产品描述

JNJ-5207852 is a novel, non-imidazole histamine H3 receptor antagonist, with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor.

靶点活性

rat H3R,8.9 (pKi)

human H3R,9.24 (pKi)

体外活性

体内活性

JNJ-5207852 is a potent dibasic amine antagonist that binds potently to rat H3 receptors (Ki=1.2 nm), and has good brain penetration. In ex vivo binding studies in mice, the compound had an ED50 of 0.13 mg kg−1, subcutaneously. It promotes wakefulness in rodents at 10 mg kg−1 s.c. but not at 1 mg kg−1, and significantly, this effect was absent in H3 receptor KO mice. JNJ-10181457 is also a dibasic amine antagonist that exhibits high-affinity binding for the rat H3 receptor (Ki=7.1 nm), promoting wakefulness in rodents and reducing cataplectic attacks in narcoleptic dogs . JNJ-10181457 improved cognitive performance in SHR pups at 10 mg kg−1[1].

化学信息

分子量

316.48

分子式

C20H32N2O

CAS

398473-34-2

溶解度

DMSO: 77.5 mg/mL (244.88 mM)

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

储存条件

store at -80°C

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 3.16 ml 15.799 ml 31.598 ml
5 mM 0.632 ml 3.16 ml 6.32 ml
10 mM 0.316 ml 1.58 ml 3.16 ml
50 mM 0.063 ml 0.316 ml 0.632 ml
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