Cayman Chemical | AH 23848 (calcium salt, hydrate)

19023 AH 23848 (calcium salt, hydrate)

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• See more Receptor Antagonist; Atherosclerosis; Bone-Related Research; Cancer; Inflammation

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Thromboxane (TXA₂) activates the T prostanoid (TP) receptor. Prostaglandin E₂ (PGE₂) activates four E prostanoid (EP) receptors, EP_1-4. AH-23848 is a dual antagonist of TP¹ and EP₄ receptors.² It originally was found to inhibit TXA₂-induced platelet aggregation (IC₅₀ = 0.26 μM)¹ and the contraction of human bronchial smooth muscle induced by the TP agonist U-46619.³ AH-23848 was subsequently demonstrated to impair PGE₂-mediated relaxation of piglet saphenous vein by antagonizing the PGE₂ receptor EP₄.² By inhibiting EP₄, it likewise suppresses serum-induced cAMP generation, cyclin A synthesis, and the proliferation of fibroblasts⁴, as well as reduces metastasis in a murine model of metastatic breast cancer.⁵

1 Brittain, R.T., Boutal, L., Carter, M.C., et al. AH23848: A thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A₂. Circulation 72 1208-1218 (1985).

2 Coleman, R.A., Grix, S.P., Head, S.A., et al. A novel inhibitory prostanoid receptor in piglet saphenous vein. Prostaglandins 47 151-168 (1994).

3 Coleman, R.A., Sheldrick, R.L.G. Prostanoid-induced contraction of human bronchial smooth muscle is mediated by TP-receptors. Br J Pharmacol 96 688-692 (1989).

4 Sanchez, T., Moreno, J.J. Role of EP₁ and EP₄ PGE₂ subtype receptors in serum-induced 3T6 fibroblast cycle progression and proliferation. Am J Physiol Cell Physiol 282 C₂₈₀-C₂₈₈ (2002).

5 ma, X., Kundu, N., Rifat, S., et al. Prostaglandin E receptor EP₄ antagonism inhibits breast cancer metastasis. Cancer Res 66(6) 2923-2927 (2006).

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Pricing updated 2010-03-18.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.