Eletriptan hydrobromide
Based on 1 publication(s) in Google Scholar
Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT1B and 5-HT1D receptor agonist with antimigraine activity, with Ki of 0.92 nM and 3.14 nM, respectively.
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- Purity: 99.33%
- CAS No.: 177834-92-3
- 화학식: C22H27BrN2O2S
- 분자량:463.43
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Eletriptan hydrobromide
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT1B Receptor |
5-HT1D Receptor |
5-HT1B Receptor 0.92 nM (Ki) |
5-HT1D Receptor 3.14 nM (Ki) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 177834-92-3
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Appearance Solid
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분자량 463.43
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화학식 C22H27BrN2O2S
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Color Off-white to light brown
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SMILES
O=S(CCC1=CC2=C(NC=C2C[C@@H]3N(CCC3)C)C=C1)(C4=CC=CC=C4)=O.Br
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Synonyms
Eletriptan HBr; UK-116044 hydrobromide
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Headache Pain
Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action. [Abstract]2024 Oct 30;25(1):187. PMID: 39478486
용액&용해도
DMSO : 100 mg/mL (215.78 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.75 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Napier C, et al. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol, 1999, 368(2-3), 259-268. [Content Brief]
[2]. MaassenVanDenBrink A, et al. Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels. Neurology, 2000, 55(10), 1524-1530. [Content Brief]
[3]. Gupta P, et al. The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist. Eur J Pharmacol, 2000, 398(1), 73-81. [Content Brief]
[4]. Hoskin KL, et al. The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res, 2004, 998(1), 91-99. [Content Brief]
[5]. Willems E, et al. Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1998, 358: 212-219. [Content Brief]
[6]. Johnson D E, et al. Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain[J]. European journal of pharmacology, 2001, 425(3): 203-210. [Content Brief]
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 (sealed storage, away from moisture). 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 | 2.1578 mL | 10.7891 mL | 21.5782 mL | 53.9456 mL |
| 5 mM | 0.4316 mL | 2.1578 mL | 4.3156 mL | 10.7891 mL | |
| 10 mM | 0.2158 mL | 1.0789 mL | 2.1578 mL | 5.3946 mL | |
| 15 mM | 0.1439 mL | 0.7193 mL | 1.4385 mL | 3.5964 mL | |
| 20 mM | 0.1079 mL | 0.5395 mL | 1.0789 mL | 2.6973 mL | |
| 25 mM | 0.0863 mL | 0.4316 mL | 0.8631 mL | 2.1578 mL | |
| 30 mM | 0.0719 mL | 0.3596 mL | 0.7193 mL | 1.7982 mL | |
| 40 mM | 0.0539 mL | 0.2697 mL | 0.5395 mL | 1.3486 mL | |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4316 mL | 1.0789 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3596 mL | 0.8991 mL | |
| 80 mM | 0.0270 mL | 0.1349 mL | 0.2697 mL | 0.6743 mL | |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5395 mL |
Eletriptan hydrobromide Related Classifications
HY-A0010 Related Classifications
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