A selective antagonist of EP4 (Ki = 3.2 nM) that less potently binds EP2 (Ki = 630 nM) and has no affinity for EP1 or EP3; delays the healing of gastric ulcers

CJ-42794 – 10 mg

Brand:
Cayman
CAS:
847728-01-2
Storage:
-20
UN-No:
Non-Hazardous - /

Prostaglandin E2 (PGE2) 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, cancer, and atherosclerosis.{16772,16773,16619} CJ-42794 is a selective antagonist of EP4 (Ki = 3.16 nM) that less potently binds EP2 (Ki = 631 nM) and has no affinity for EP1 or EP3.{14996,26030} It has minimal effect on numerous other receptors, enzymes, or channels.{26030} Unlike general inhibitors of PGE2 synthesis, CJ-42794 does not cause damage to rat gastrointestinal mucosa.{14996} Instead, it delays the healing of gastric ulcers in mice and rats, suppressing the upregulation of VEGF expression and angiogenesis.{26032} CJ-42794 blocks pain and inflammation in rat models of arthritis as well as gastric tumorigenesis in mice.{25895,26031}  

 

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Description

A selective antagonist of EP4 (Ki = 3.2 nM) that less potently binds EP2 (Ki = 630 nM) and has no affinity for EP1 or EP3; delays the healing of gastric ulcers, suppressing the upregulation of VEGF expression and angiogenesis; blocks pain and inflammation in rat models of arthritis and gastric tumorigenesis in mice

Formal name: 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]-benzoic acid

Synonyms:  RQ-00015986

Molecular weight: 413.8

CAS: 847728-01-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Angiogenesis||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Gastric Disease|Peptic Ulcers||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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