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E7046 (ER-886406) Prostaglandin Receptor inhibitor

Name: E7046 (ER-886406)
Brand: Selleck Chemicals
SKU: S6649
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6649

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.

Chemical Structure

Molecular Weight: 483.39

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.80

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Prostaglandin Receptor Inhibitors	PF-04418948 TG4-155 Grapiprant (CJ-023,423) BI-671800 Setipiprant (ACT-129968) Terutroban Genz-123346 free base EP4-IN-1 Ozagrel (-)-(S)-α-terpineol

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (206.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/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.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/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.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	483.39	Formula	C₂₂H₁₈F₅N₃O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1369489-71-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Palupiprant, AN0025			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

Mechanism of Action

Targets/IC₅₀/Ki	EP4 (Cell-free assay) 13.5nM EP4 (Cell-free assay) 23.14 nM(Ki)
In vitro	E7046 has specific and potent inhibitory activity on PGE₂-mediated pro-tumor myeloid cell differentiation and activation.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28920002/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02540291	Terminated	Tumors	Eisai Inc.	July 30 2015	Phase 1

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