2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. EP4 receptor antagonist 8

EP4 receptor antagonist 8 is an orally active EP4 antagonist (human EP4 IC50 = 6.40 nM). EP4 receptor antagonist 8 significantly reduced paw and joint swelling, inflammatory cell infiltration, cartilage damage, pannus formation, and joint bone erosion in arthritis (AIA) mice in a dose-dependent manner. EP4 receptor antagonist 8 can be used for the study of inflammatory pain.

For research use only. We do not sell to patients.

EP4 receptor antagonist 8

EP4 receptor antagonist 8 Chemical Structure

CAS No. : 3068255-86-4

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

EP4 receptor antagonist 8 Related Antibodies

Top Publications Citing Use of Products

View All Prostaglandin Receptor Isoform Specific Products:

View All Isoforms
DP EP FP IP TXA2/TP TXB2

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EP4 receptor antagonist 8 is an orally active EP4 antagonist (human EP4 IC50 = 6.40 nM). EP4 receptor antagonist 8 significantly reduced paw and joint swelling, inflammatory cell infiltration, cartilage damage, pannus formation, and joint bone erosion in arthritis (AIA) mice in a dose-dependent manner. EP4 receptor antagonist 8 can be used for the study of inflammatory pain[1].

IC50 & Target

EP4

6.4 nM (IC50)

IL-6

 

In Vitro

EP4 receptor antagonist 8's (Compound 27i) (100 μg/mL, 0-60 min) metabolic stability in rat liver microsomes (RLM) decreases over time, with a remaining percentage of 41.44% at 60 minutes[1].
EP4 receptor antagonist 8 (24 h) exhibits a moderate plasma protein binding rate at 24 h (97.60 %)[1].
EP4 receptor antagonist 8 significantly reduces IL-6 levels in a dose-dependent manner in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EP4 receptor antagonist 8 Related Antibodies

ELISA Assay[1]

Cell Line: Lipopolysaccharides (LPS)-induced RAW 264.7 cells
Concentration: 6.25 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: Pretreated 1 h, then simulated with LPS for 24 h
Result: Reduced LPS-induced IL-6 levels in a dose-dependent manner.
In Vivo

EP4 receptor antagonist 8 (Compound 27i) (5-20 mg/kg, i.p., once, performed 24 hours after CFA injection) exhibits significant anti-inflammatory and analgesic effects in a (Freund’s complete adjuvant) CFA-induced C57BL/6 mice arthritis model in a dose-dependent manner[1].
EP4 receptor antagonist 8 (5-20 mg/kg, p.o., once daily for 5 days) exhibits potent anti-inflammatory activity in a Kunming mouse acute inflammation model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Chronic arthritis was induced in the right hind paw using C57BL/6 mice (female, weighing 20-22 g) by injection of complete Freund's adjuvant (CFA)[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: I.p., once, performed 24 hours after CFA injection
Result: Significantly improved the swelling of mice paws in a dose-dependent manner.
Increased the pain threshold; in both the hot plate test and the Von Frey test, the 20 mg/kg group showed the best effect within 120 minutes.
Reduced joint inflammation, cartilage damage, bone erosion, and pannus formation.
Reduced IL-1β, IL-6, and TNF-α positive cells in joint tissue.
Animal Model: Acute ear inflammation and swelling were induced in male Kunming mice (weighing 20-22 g) by uniformly applying xylene (20 μL) to the right ear[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: P.o., once daily for 5 days
Result: Showed excellent inhibitory effect, and the inhibitory rate was as high as 47.09 %, which was dose-dependent.
Molecular Weight

516.94

Formula

C26H21ClN6O4
CAS No.
SMILES

O=C(O)C1=CC=C(CNC(C2=C3C=CC=CC3=NN2CCNC(NC4=CC=C(C#N)C=C4Cl)=O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EP4 receptor antagonist 8 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EP4 receptor antagonist 83068255-86-4Prostaglandin ReceptorInterleukin RelatedILAnalgesic activityAnti-inflammatoryEP4 antagonistsStructure activity relationshipInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EP4 receptor antagonist 8
Cat. No.:
HY-178465
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.