Enerisant
Based on 1 Customer Validation
Enerisant (TS-091) 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.79%
- No. CAS: 1152747-82-4
- Fòrmula: C22H30N4O3
- Peso molecular:398.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
IC50: 2.89 nM (human histamine H3 receptor), 14.5 nM (rat histamine H3 receptor)
Ki: 1.65 nM (human histamine H3 receptor), 7.87 nM (rat histamine H3 receptor)[1]
Enerisant hydrochloride (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 hydrochloride (1 mg/kg; s.c.; once) increases the total extracellular histamine levels in the posterior hypothalamus in rats[1].
Enerisant hydrochloride (1 mg/kg; i.p.; once) increases the total extracellular dopamine and acetylcholine levels in the medial prefrontal cortex (mPFC) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rats, R-α-methylhistamine-induced dipsogenia model[1]
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Dosage:0.1, 0.3 and 1 mg/kg
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Administration:Oral, single dose
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Result:Attenuated the dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1152747-82-4
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Appearance Solid
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Peso molecular 398.50
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Fòrmula C22H30N4O3
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Color Off-white to light yellow
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SMILES
O=C(C1=CN(C2=CC=C(OCCCN3[C@H](C)CCC3)C=C2)N=C1)N4CCOCC4
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Synonyms
TS-091
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (250.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5094 mL | 12.5471 mL | 25.0941 mL | 62.7353 mL |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL | 12.5471 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 mL | 6.2735 mL | |
| 15 mM | 0.1673 mL | 0.8365 mL | 1.6729 mL | 4.1824 mL | |
| 20 mM | 0.1255 mL | 0.6274 mL | 1.2547 mL | 3.1368 mL | |
| 25 mM | 0.1004 mL | 0.5019 mL | 1.0038 mL | 2.5094 mL | |
| 30 mM | 0.0836 mL | 0.4182 mL | 0.8365 mL | 2.0912 mL | |
| 40 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5684 mL | |
| 50 mM | 0.0502 mL | 0.2509 mL | 0.5019 mL | 1.2547 mL | |
| 60 mM | 0.0418 mL | 0.2091 mL | 0.4182 mL | 1.0456 mL | |
| 80 mM | 0.0314 mL | 0.1568 mL | 0.3137 mL | 0.7842 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2509 mL | 0.6274 mL |
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