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Eplivanserin

Name: Eplivanserin
Brand: TargetMol
SKU: T11217
Price: 195 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

🥰Excellent

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 Size	Price	Availability
1 mg	$195	In Stock
5 mg	$437	In Stock
10 mg	$646	In Stock
25 mg	$987	In Stock
50 mg	$1,380	In Stock
1 mL x 10 mM (in DMSO)	$443	In Stock

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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:5.8 nM (in rat cortical membrane), 5-HT2C receptor:120 nM, 5-HT2 receptor:1.14 nM (Ki)
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].
Synonyms	SR-46349

Chemical Properties

Molecular Weight	328.38
Formula	C₁₉H₂₁FN₂O₂
Cas No.	130579-75-8
Smiles	CN(C)CCO\N=C(\C=Cc1ccc(O)cc1)c1ccccc1F
Relative Density.	1.08
Color	Yellow
Appearance	Solid

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (152.26 mM), Sonication is recommended.

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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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.

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