A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC50 = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein

AH 23848 (calcium salt) – 1 mg

Brand:
Cayman
CAS:
81496-19-7
Storage:
-20
UN-No:
Non-Hazardous - /

Thromboxane (TXA2) activates the T prostanoid (TP) receptor. Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. AH-23848 is a dual antagonist of TP{3339} and EP4 receptors.{1755} It originally was found to inhibit TXA2-induced platelet aggregation (IC50 = 0.26 μM){3339} and the contraction of human bronchial smooth muscle induced by the TP agonist U-46619.{1756} AH-23848 was subsequently demonstrated to impair PGE2-mediated relaxation of piglet saphenous vein by antagonizing the PGE2 receptor EP4.{1755} By inhibiting EP4, it likewise suppresses serum-induced cAMP generation, cyclin A synthesis, and the proliferation of fibroblasts{16771}, as well as reduces metastasis in a mouse model of metastatic breast cancer.{14694}  

 

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Description

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC50 = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a mouse model of breast cancer

Formal name: (4Z)-rel-7-[(1R,2R,5S)-5-([1,1′-biphenyl]-4-ylmethoxy)-2-(4-morpholinyl)-3-oxocyclopentyl]-4-heptenoic acid, hemicalcium salt

Synonyms: 

Molecular weight: 496.6

CAS: 81496-19-7

Purity: ≥90%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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