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Eplivanserin

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Catalog No. T11217Cas No. 130579-75-8
Alias SR-46349

Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.

Eplivanserin

Eplivanserin

😃Good
Catalog No. T11217Alias SR-46349Cas No. 130579-75-8
Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.
Pack SizePriceAvailabilityQuantity
1 mg$1956-8 weeks
5 mg$4376-8 weeks
10 mg$6466-8 weeks
25 mg$9876-8 weeks
50 mg$1,3806-8 weeks
1 mL x 10 mM (in DMSO)$4436-8 weeks
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Product Introduction

Bioactivity
Description
Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.
Targets&IC50
5-HT2 receptor:1.14 nM (ki), 5-HT2 receptor:5.8 nM (in rat cortical membrane)
In vitro
Eplivanserin has inhibitory effects on rat cortex adrenergic α1 and α2, rat whole brain histammine H1, Na+ channel, and rat striatum dopamine D1 and D2, with IC50s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C with IC50s of 0.12 μM (Pig cortex 5-HT1C), 14 μM (Rat hippocampus 5-HT1A), and 16 μM (Rat stnatum 5-HT1B, Ox caudate nucleus 5-HT1D)[1].
In vivo
In mice, Eplivanserin(0.097 mg/kg; i.p.) inhibits 5-HT2 receptor binding of [3H]ketanserin with an ED50 of 0.087 mg/kg[1]. In rats, SR 46349B (0.25-1 mg/kg; i.p.) blocks Cocaine-evoked hyperactivity following repeated Cocaine treatment[2].
AliasSR-46349
Chemical Properties
Molecular Weight328.38
FormulaC19H21FN2O2
Cas No.130579-75-8
Relative Density.1.08
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (152.26 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0453 mL15.2263 mL30.4525 mL152.2626 mL
5 mM0.6091 mL3.0453 mL6.0905 mL30.4525 mL
10 mM0.3045 mL1.5226 mL3.0453 mL15.2263 mL
20 mM0.1523 mL0.7613 mL1.5226 mL7.6131 mL
50 mM0.0609 mL0.3045 mL0.6091 mL3.0453 mL
100 mM0.0305 mL0.1523 mL0.3045 mL1.5226 mL

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