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JNJ-5207852

Catalog No. T7413 CAS 398473-34-2

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.

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JNJ-5207852, CAS 398473-34-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 473.00
100 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 98%

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Description	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.
Targets&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].

Molecular Weight	316.48
Formula	C20H32N2O
CAS No.	398473-34-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 77.5 mg/mL (244.88 mM)

References and Literature

1. Esbenshade T A , Browman K E , Bitner R S , et al. The histamine H3 receptor: an attractive target for the treatment of cognitive disorders[J]. 2008, 154(6):1166-1181. 2. Abuhamdah R M A , Ruan V R , Lethbridge N L , et al. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze[J]. Frontiers in Systems Neuroscience, 2012, 6.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compounds Library Max Anti-Parkinson's Disease Compound Library Bioactive Compound Library ReFRAME Related Library Immunology/Inflammation Compound Library Neurotransmitter Receptor Compound Library Histamine & Melatonin Receptor-Targeted Compound Library

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Keywords

JNJ-5207852 398473-34-2 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor sleep low JNJ5207852 Inhibitor REM toxicity JNJ 5207852 inhibit inhibitor

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