Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | H3 receptor (rat):8.9 (pKi) , H3 receptor (human):9.24 (pKi) |
In vivo | 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]. |
分子量 | 316.48 |
分子式 | C20H32N2O |
CAS No. | 398473-34-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 77.5 mg/mL (244.88 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
JNJ-5207852 398473-34-2 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor sleep low JNJ5207852 Inhibitor REM toxicity JNJ 5207852 inhibit inhibitor