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: 1369489-71-3

Selleck's E7046 (ER-886406) has been cited by 1 publication

Purity & Quality Control

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

E7046 (ER-886406) Related Products

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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.)


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In vivo
Batch:

Add solvents to the product individually and in order.


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In vivo Formulation Calculator (Clear solution)

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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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