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JNJ-5207852
Catalog No. T7413Cas No. 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.
JNJ-5207852
Catalog No. T7413Cas No. 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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $43 | In Stock | |
| 10 mg | $68 | In Stock | |
| 25 mg | $143 | In Stock | |
| 50 mg | $283 | In Stock | |
| 100 mg | $416 | In Stock | |
| 200 mg | $592 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $47 | In Stock |
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 77.5 mg/mL (244.88 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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