Art. -Nr.: HY-A0010

Eletriptan hydrobromide

(Synonyms: Eletriptan HBr; UK-116044 hydrobromide)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT_1B and 5-HT_1D receptor agonist with antimigraine activity, with K_i of 0.92 nM and 3.14 nM, respectively.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.33%
CAS. Nr.: 177834-92-3
Formel: C₂₂H₂₇BrN₂O₂S
Molecular Weight:463.43

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Eletriptan hydrobromide Chemical Structure

CAS. Nr.: 177834-92-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT_1B and 5-HT_1D receptor agonist with antimigraine activity, with K_i of 0.92 nM and 3.14 nM, respectively^[1]^[2]^[3]^[4]^[5]^[6].

IC₅₀ & Target^[1]

5-HT_1B Receptor

5-HT_1D Receptor

5-HT_1B Receptor

0.92 nM (Ki)

5-HT_1D Receptor

3.14 nM (Ki)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

Eletriptan (1-1000 μg/kg; i.v.; after a 60-minute stabilization period, dosed at 5-minute intervals with readings taken every 30 seconds) hydrobromide dose-dependently reduces carotid blood flow in anesthetized dogs^[1].
Eletriptan (30-300 μg/kg; i.v.) hydrobromide dose-dependently inhibits dural plasma protein extravasation in anesthetized rats and rapidly and completely inhibits plasma protein extravasation from the dura mater at a dose of 100 μg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 177834-92-3
Appearance Solid
Molecular Weight 463.43
Formel C₂₂H₂₇BrN₂O₂S
Color Off-white to light brown
SMILES

O=S(CCC1=CC2=C(NC=C2C[C@@H]3N(CCC3)C)C=C1)(C4=CC=CC=C4)=O.Br
Synonyms

Eletriptan HBr; UK-116044 hydrobromide
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

All

Sort by:

Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1578 mL

10.7891 mL

21.5782 mL

5 mM

0.4316 mL

2.1578 mL

4.3156 mL

10 mM

0.2158 mL

1.0789 mL

2.1578 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Eletriptan hydrobromide

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Eletriptan hydrobromide

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Obesity Compound Library

Antidepressant Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Eletriptan hydrobromide

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eletriptan hydrobromide Related Classifications

HY-A0010 Related Classifications