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Etrasimod

Name: Etrasimod
Brand: TargetMol
SKU: TQ0227
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0227Cas No. 1206123-37-6

Alias APD334

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).

Etrasimod

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Purity: 99.73%

Catalog No. TQ0227Alias APD334Cas No. 1206123-37-6

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$189	In Stock	In Stock
25 mg	$255	In Stock	In Stock
50 mg	$322	In Stock	In Stock
100 mg	$446	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$115	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.73%

Appearance:Solid

Color:White to Brown

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).
Targets&IC50	S1P1:1.88 nM (CHO cells)
In vitro	In CHO cells expressing HA-tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3.
In vivo	APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmax across all species. In both dog and monkey, a significant decrease in the volume of distribution (Vss) is observed relative to the rodent. Oral bioavailability is in the range of 40–100% and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in the dog.
Animal Research	APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose. APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose.
Synonyms	APD334

Chemical Properties

Molecular Weight	457.48
Formula	C₂₆H₂₆F₃NO₃
Cas No.	1206123-37-6
Smiles	OC(=O)C[C@H]1CCc2c1[nH]c1ccc(OCc3ccc(C4CCCC4)c(c3)C(F)(F)F)cc21
Relative Density.	1.326 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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: 25 mg/mL (54.65 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1859 mL	10.9294 mL	21.8589 mL	109.2944 mL
5 mM	0.4372 mL	2.1859 mL	4.3718 mL	21.8589 mL
10 mM	0.2186 mL	1.0929 mL	2.1859 mL	10.9294 mL
20 mM	0.1093 mL	0.5465 mL	1.0929 mL	5.4647 mL
50 mM	0.0437 mL	0.2186 mL	0.4372 mL	2.1859 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