A selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors) that has been shown to inhibit inflammation without gastrointestinal toxicity in various animal models for arthritis

MF498 – 5 mg

Brand:
Cayman
CAS:
915191-42-3
Storage:
-20
UN-No:
Non-Hazardous - /

Prostaglandin E2 (PGE2; Item No. 14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}  

 

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Description

A selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors) that has been shown to inhibit inflammation without gastrointestinal toxicity in various animal models for arthritis

Formal name: N-[[[4-(5,9-diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide

Synonyms: 

Molecular weight: 603.7

CAS: 915191-42-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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