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Eletriptan hydrobromide

Name: Eletriptan hydrobromide
Brand: TargetMol
SKU: T0216
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0216Cas No. 177834-92-3

Alias UK-116044, Eletriptan HBr

Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor.

Eletriptan hydrobromide

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Purity: 99.85%

Catalog No. T0216Alias UK-116044, Eletriptan HBrCas No. 177834-92-3

Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$33	In Stock	In Stock
5 mg	$52	In Stock	In Stock
10 mg	$64	In Stock	In Stock
25 mg	$136	In Stock	In Stock
50 mg	$228	In Stock	In Stock
100 mg	$379	In Stock	In Stock
200 mg	$559	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$57	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.85%

Color:White

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COA

Product Introduction

Bioactivity

Description	Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor.
Targets&IC50	5-HT1B:0.92 nM(Ki), 5-HT1D:3.14 nM(Ki)
In vitro	[3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan). [1] Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery. [2]
In vivo	The total number of binding sites (Bmax) of [3H]Eletriptan to 5-HT1B and 5-HT1D was 2478 fmol/mg and 1576 fmol/mg, respectively.The binding rate of [3H]Eletriptan (K(on) 0.249/min/nM) was significantly faster than that of [3H]sumatriptan (K(on) 0.024/ min/nM), while the shedding rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) was significantly slower than [3H]Eletriptan . [1] Eletriptan induces concentration-dependent constriction in meningeal arteries, coronary arteries, and saphenous veins.Eletriptan is more potent in meningeal arteries than in coronary arteries (86-fold) or saphenous veins (66-fold). The predicted contractility of Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C (max) in meningeal arteries observed in clinical trials is similar. [2]
Synonyms	UK-116044, Eletriptan HBr

Chemical Properties

Molecular Weight	463.43
Formula	C₂₂H₂₇BrN₂O₂S
Cas No.	177834-92-3
Smiles	Br.CN1CCC[C@@H]1Cc1c[nH]c2ccc(CCS(=O)(=O)c3ccccc3)cc12
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (129.47 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.32 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1578 mL	10.7891 mL	21.5782 mL	107.8912 mL
5 mM	0.4316 mL	2.1578 mL	4.3156 mL	21.5782 mL
10 mM	0.2158 mL	1.0789 mL	2.1578 mL	10.7891 mL
20 mM	0.1079 mL	0.5395 mL	1.0789 mL	5.3946 mL
50 mM	0.0432 mL	0.2158 mL	0.4316 mL	2.1578 mL
100 mM	0.0216 mL	0.1079 mL	0.2158 mL	1.0789 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc