Home GPCR & G Protein Prostaglandin Receptor inhibitor E7046 (ER-886406) For research use only.

E7046 (ER-886406)

Synonyms: Palupiprant, AN0025

E7046 (ER-886406, Palupiprant, AN0025) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.

E7046 (ER-886406) Chemical Structure

E7046 (ER-886406) Chemical Structure

CAS No. 1369489-71-3

Size Price Stock Quantity
5mg USD 147 In stock
25mg USD 370 In stock
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Purity & Quality Control

Batch: S664901 DMSO]100 mg/mL]false]]]false]]]false Purity: 99.80%
99.80

E7046 (ER-886406) Related Products

Biological Activity

Description E7046 (ER-886406, Palupiprant, AN0025) is a selective inhibitor of the prostaglandin E2 (PGE2) receptor EP4 with IC50 of 13.5 nM and Ki of 23.14 nM.
Targets
EP4 [1]
(Cell-free assay)		 EP4 [1]
(Cell-free assay)
13.5nM 23.14 nM(Ki)
In vitro
In vitro

E7046 has specific and potent inhibitory activity on PGE2-mediated pro-tumor myeloid cell differentiation and activation.[1]
Cell Research Cell lines Monocytes
Concentrations 10,100,300,1000,or 3000 nM
Incubation Time 7d
Method

Monocytes are placed in culture with recombinant human GM-CSF (20 ng/mL) + human IL-4 (500 U/mL) ± PGE2 (10 nM) ± E7046 (10,100,300,1000,or 3000 nM) for 7 d.
In Vivo
In vivo

E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8+ T cells.[1]
Animal Research Animal Models C57BL/6 mice
Dosages 100 mg/kg or 150 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02540291 Terminated
Tumors
Eisai Inc.
 July 30 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 483.39 Formula

C22H18F5N3O4
CAS No. 1369489-71-3 SDF --
Smiles CC(C1=CC=C(C=C1)C(=O)O)NC(=O)C2=C(N(N=C2C(F)F)C)OC3=CC=CC(=C3)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (206.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator
Clear solution
5% DMSO 95% Corn oil
5.0mg/ml (10.34mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40% 5% 50%ddH2O
5.0mg/ml (10.34mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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