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AH 23848 (calcium salt, hydrate)

Cayman Chemical Item Number 19023

AH 23848 (calcium salt, hydrate)

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Description

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 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 mouse 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., and 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., and 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).

Formal Name 7-​[5α-​([1S,​1α(Z)-​biphenyl]-​4-​ylmethoxy)-​2β-​(4-​morpholinyl)-​3-​oxocyclopentyl]-​4-​heptenoic acid,​ calcium salt,​ hydrate
Molecular Formula [C29H34NO5]2 Ca2+ · XH2O
Formula Weight 1011.3
Formulation A crystalline solid
Purity ≥90%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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OC(=O)​CC/C=C\CCC1C(OCc2ccc(cc2)​c2ccccc2)​CC(=O)​[C@H]​1N1CCOCC1

Background Reading

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

Sanchez, T., and 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).

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

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).

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).

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Size Price Quantity Subtotal
1 mg $65.00 $0.00
5 mg $293.00 $0.00
10 mg $520.00 $0.00
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Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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