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Eletriptan hydrobromide

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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

Eletriptan hydrobromide

🥰Excellent
Purity: 100%
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 SizePriceAvailabilityQuantity
2 mg$33In Stock
5 mg$52In Stock
10 mg$64In Stock
25 mg$136In Stock
50 mg$247In Stock
100 mg$450In Stock
200 mg$585In Stock
500 mg$937In Stock
1 mL x 10 mM (in DMSO)$57In Stock
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Purity:100%
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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]
AliasUK-116044, Eletriptan HBr
Chemical Properties
Molecular Weight463.43
FormulaC22H27BrN2O2S
Cas No.177834-92-3
SmilesBr.CN1CCC[C@@H]1Cc1c[nH]c2ccc(CCS(=O)(=O)c3ccccc3)cc12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (129.47 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1578 mL10.7891 mL21.5782 mL107.8912 mL
5 mM0.4316 mL2.1578 mL4.3156 mL21.5782 mL
10 mM0.2158 mL1.0789 mL2.1578 mL10.7891 mL
20 mM0.1079 mL0.5395 mL1.0789 mL5.3946 mL
50 mM0.0432 mL0.2158 mL0.4316 mL2.1578 mL
100 mM0.0216 mL0.1079 mL0.2158 mL1.0789 mL

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