EP4 receptor antagonist 8

Name: EP4 receptor antagonist 8
Brand: TargetMol
SKU: T213334
Rating: 4.5 (1 reviews)

Catalog No. T213334 Copy Product Info

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EP4 receptor antagonist 8 is an orally active EP4 receptor antagonist with an IC50 value of 6.40 nM in humans. This compound significantly reduces paw and joint swelling, infiltration of inflammatory cells, cartilage damage, pannus formation, and bone erosion in a dose-dependent manner in arthritis (AIA) mice. EP4 receptor antagonist 8 is useful for research on inflammatory pain.

EP4 receptor antagonist 8

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Catalog No. T213334

EP4 receptor antagonist 8

Cas No. 3068255-86-4

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	EP4 receptor antagonist 8 is an orally active EP4 receptor antagonist with an IC50 value of 6.40 nM in humans. This compound significantly reduces paw and joint swelling, infiltration of inflammatory cells, cartilage damage, pannus formation, and bone erosion in a dose-dependent manner in arthritis (AIA) mice. EP4 receptor antagonist 8 is useful for research on inflammatory pain.
Targets&IC50	EP4:6.4 nM
In vitro	EP4 receptor antagonist 8 (Compound 27i) shows a time-dependent decrease in metabolic stability in rat liver microsomes (RLM), with a remaining percentage of 41.44% at 60 minutes when tested at 100 μg/mL. Over 24 hours, it exhibits a moderate plasma protein binding rate of 97.60%. Additionally, EP4 receptor antagonist 8 significantly reduces IL-6 levels in LPS-induced RAW 264.7 cells in a dose-dependent manner.
In vivo	EP4 receptor antagonist 8 (Compound 27i) administered intraperitoneally at doses of 5-20 mg/kg as a single dose 24 hours after CFA injection, demonstrates significant anti-inflammatory and analgesic effects in a dose-dependent manner in a CFA-induced arthritis model in C57BL/6 mice. Additionally, when given orally at 5-20 mg/kg once daily for 5 days, it exhibits potent anti-inflammatory activity in an acute inflammation model in Kunming mice.

Chemical Properties

Molecular Weight	516.94
Formula	C₂₆H₂₁ClN₆O₄
Cas No.	3068255-86-4
Smiles	N#CC1=CC=C(NC(=O)NCCN2N=C3C=CC=CC3=C2C(=O)NCC4=CC=C(C=C4)C(=O)O)C(Cl)=C1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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.

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