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.
- CAS No.: 3068255-86-4
- Formula: C26H21ClN6O4
- Molecular Weight:516.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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EP4 6.4 nM (IC50) |
IL-6 |
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.
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Cell Line:Lipopolysaccharides (LPS)-induced RAW 264.7 cells
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Concentration:6.25 μM, 12.5 μM, 25 μM, 50 μM
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Incubation Time:Pretreated 1 h, then simulated with LPS for 24 h
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Result:Reduced LPS-induced IL-6 levels in a dose-dependent manner.
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.
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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].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:I.p., once, performed 24 hours after CFA injection
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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.
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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].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:P.o., once daily for 5 days
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Result:Showed excellent inhibitory effect, and the inhibitory rate was as high as 47.09 %, which was dose-dependent.
Chemical Information
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CAS No. 3068255-86-4
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Molecular Weight 516.94
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Formula C26H21ClN6O4
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SMILES
O=C(O)C1=CC=C(CNC(C2=C3C=CC=CC3=NN2CCNC(NC4=CC=C(C#N)C=C4Cl)=O)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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