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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%

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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-HT1D:3.14 nM(Ki), 5-HT1B:0.92 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

Powder: -20°C for 3 years | 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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