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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

😃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 Size	Price	USA Warehouse	Global Warehouse
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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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Appearance:Solid

Color:Yellow

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COA

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-HT2C receptor:120 nM, 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].
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

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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc