Enerisant (Synonyms: TS-091) |
カタログ番号GC74093
One-Click Copy Product Info
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Enerisantは強力で選択的で競争的で経口活性のヒスタミンH 3受容体アンタゴニスト/逆アゴニストであり、ヒトとラットヒスタミンH 3受容体のIC 50はそれぞれ2.89 nMと14.5 nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1152747-82-4
Sample solution is provided at 25 µL, 10mM.
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Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
Enerisant drochloride (0.3-1 mg/kg; p.o.; once) attenuats the dipsogenia response in rats[1].Enerisant drochloride (0.1-3 mg/kg; p.o.; once) results in the occupancy of the histamine H3 receptor in a dose-dependent manner in rats. A dose eliciting a half-maximal receptor occupancy is 0.78 mg/kg[1].Enerisant drochloride (1 mg/kg; s.c.; once) increases the total extracellular histamine levels in the posterior pothalamus in rats[1].Enerisant drochloride (1 mg/kg; i.p.; once) increases the total extracellular dopamine and acetylcholine levels in the medial prefrontal cortex (mPFC) in rats[1].
References:
[1]. Hino N, et al. A novel potent and selective histamine H3 receptor antagonist enerisant: in vitro profiles, in vivo receptor occupancy, and wake-promoting and procognitive effects in rodents. Journal of Pharmacology and Experimental Therapeutics, 2020, 375(2): 276-285.
| Cas No. | 1152747-82-4 | SDF | |
| 同義語 | TS-091 | ||
| Formula | C22H30N4O3 | M.Wt | 398.5 |
| 溶解度 | DMSO : 100 mg/mL (250.94 mM; Need ultrasonic) | Storage | -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. |
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| 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 | 2.5094 mL | 12.5471 mL | 25.0941 mL |
| 5 mM | 501.9 μL | 2.5094 mL | 5.0188 mL |
| 10 mM | 250.9 μL | 1.2547 mL | 2.5094 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 saline, 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)