Bavisant dihydrochloride hydrate (Synonyms: JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate) |
| Catalog No.GC35473 |
Bavisant dihydrochloride hydrate (JNJ31001074AAC)는 히스타민 H3 수용체의 경구 활성, 강력한 뇌 침투 및 고도로 선택적인 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1103522-80-0
Sample solution is provided at 25 µL, 10mM.
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Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1 mg/day, 3 mg/day and 10 mg/day groups, respectively; the change in the 10 mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1 mg/day and 3 mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2
[1]. Robert L. Hudkins, Rita Raddatz, Ming Tao, Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant):A Potent, Selective Histamine H3 Receptor Inverse Agonist. J. Med. Chem. 2011, 54, 4781-4792 [2]. Weisler RH, Pandina GJ, Daly EJ, Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
| Cas No. | 1103522-80-0 | SDF | |
| Synonyms | JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate | ||
| Canonical SMILES | O=C(N1CCN(C2CC2)CC1)C(C=C3)=CC=C3CN4CCOCC4.[H]Cl.[H]Cl.O | ||
| Formula | C19H31Cl2N3O3 | M.Wt | 420.37 |
| Solubility | Water: ≥ 50 mg/mL (118.94 mM); DMSO: ≥ 1 mg/mL (2.38 mM) | Storage | Store at -20°C |
| 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 | 2.3789 mL | 11.8943 mL | 23.7886 mL |
| 5 mM | 475.8 μL | 2.3789 mL | 4.7577 mL |
| 10 mM | 237.9 μL | 1.1894 mL | 2.3789 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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