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Eplivanserin

Catalog No. T11217Cas 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.

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Pack Size	Price	Availability
1 mg	$195	6-8 weeks
5 mg	$437	6-8 weeks
10 mg	$646	6-8 weeks
25 mg	$987	6-8 weeks
50 mg	$1,380	6-8 weeks
1 mL x 10 mM (in DMSO)	$443	6-8 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.
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].
Alias	SR-46349

Chemical Properties

Molecular Weight	328.38
Formula	C19H21FN2O2
Cas No.	130579-75-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (152.26 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0453 mL	15.2263 mL	30.4525 mL	152.2626 mL
5 mM	0.6091 mL	3.0453 mL	6.0905 mL	30.4525 mL
10 mM	0.3045 mL	1.5226 mL	3.0453 mL	15.2263 mL
20 mM	0.1523 mL	0.7613 mL	1.5226 mL	7.6131 mL
50 mM	0.0609 mL	0.3045 mL	0.6091 mL	3.0453 mL
100 mM	0.0305 mL	0.1523 mL	0.3045 mL	1.5226 mL

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

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

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