JNJ 5207852 dihydrochloride |
| カタログ番号GC11046 |
JNJ 5207852 二塩酸塩は、選択的かつ強力なヒスタミン H3 受容体 (H3R) 拮抗薬であり、ラットおよびヒト H3R の pKis はそれぞれ 8.9、9.24 です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 398473-34-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
In mice and rats, JNJ-5207852 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. No rebound hypersomnolence, as measured by slow-wave delta power, is observed. The wake promoting effects of this H3 receptor antagonist are not associated with hypermotility. A 4-week daily treatment of mice with JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight, possibly due to the compound being a neutral antagonist at the H3 receptor. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels[1].
References:
[1]. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
[2]. Abuhamdah RM, 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. Front Syst Neurosci. 2012 Jul 16;6:54.
Animal experiment: | Rats[1]Male, Sprague-Dawley rats weighing 282-334 g are used. The animals are individually housed with free access to food and water. To assure that there are no pre-existing group differences in activity levels prior to the initiation of treatment, LMA is monitored and recorded during a 2 h habituation period. Following the 2 h habituation period, testing is briefly interrupted and animals are s.c. injected with either saline (1 mL/kg; n=6), JNJ-5207852 (3, 10, 30 mg/kg; n=6-7 animals/group) or Damphetamine (0.75 mg/kg; n=6). Testing is immediately resumed following the compound injection[1]. |
References: [1]. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. | |
| Cas No. | 398473-34-2 | SDF | |
| Chemical Name | 1-(4-(3-(piperidin-1-yl)propoxy)benzyl)piperidine dihydrochloride | ||
| Canonical SMILES | C1(CN2CCCCC2)=CC=C(OCCCN3CCCCC3)C=C1.Cl.Cl | ||
| Formula | C20H32N2O.2HCl | M.Wt | 389.4 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 16 mg/ml,PBS (pH 7.2): 0.25 mg/ml | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL |
| 10 mM | 0.2568 mL | 1.284 mL | 2.5681 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *