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Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $33 | In Stock | |
5 mg | $52 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $136 | In Stock | |
50 mg | $247 | In Stock | |
100 mg | $450 | In Stock | |
200 mg | $585 | In Stock | |
500 mg | $937 | In Stock | |
1 mL x 10 mM (in DMSO) | $57 | In Stock |
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] |
Alias | UK-116044, Eletriptan HBr |
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 | Powder: -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
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