AH 23848 (calcium salt)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AH 23848 (calcium salt) is a dual antagonist of TP1 and EP4 receptors [1][2].
The thromboxane receptor (TP), also known as the prostanoid TP receptor, is activated by thromboxane A2 (TXA2). TXA2 is an exceptionally potent inducer of platelet aggregation and of contraction of vascular and respiratory smooth muscle [1]. Prostaglandin E2 (PGE2) subtype receptors (EP) are involved in cellular proliferation and tumor development. Prostaglandin E2 (PGE2) activates four EP receptors, EP1-4. The EP4 receptor is coupled to Gs and mediates increases in cAMP concentration by activation of adenylyl cyclase [4].
AH 23848 (calcium salt) is a dual antagonist of TP1 and EP4 receptors. AH 23848 is an orally active, potent and specific thromboxane receptor-blocking drug that has a long duration of action. AH 23848 inhibited TXA2-induced platelet aggregation and antagonized the contraction of human bronchial smooth muscle induced by the TP agonist U-46619 with pA2 of 8.3 [1][3]. In 3T6 fibroblasts, AH-23848B induced accumulation of cells in early S phase and lowered cyclin A levels [4].
In syngeneic BALB/cByJ female mice injected with line 66.1 or 410.4 tumor cells, AH23848 inhibited the metastasis of line 66.1 and 410.4 cells [5].
References:
[1]. Brittain RT, Boutal L, Carter MC, et al. AH23848: a thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A2. Circulation. 1985 Dec;72(6):1208-18.
[2]. Coleman RA, Grix SP, Head SA, et al. A novel inhibitory prostanoid receptor in piglet saphenous vein. Prostaglandins. 1994 Feb;47(2):151-68.
[3]. Coleman RA, Sheldrick RL. Prostanoid-induced contraction of human bronchial smooth muscle is mediated by TP-receptors. Br J Pharmacol. 1989 Mar;96(3):688-92.
[4]. Sanchez, T., and Moreno, J.J. Role of EP1 and EP4 PGE2 subtype receptors in serum-induced 3T6 fibroblast cycle progression and proliferation. American Journal of Physiology.Cell Physiology 282, C280-C288 (2002).
[5]. Ma X, Kundu N, Rifat S, et al. Prostaglandin E receptor EP4 antagonism inhibits breast cancer metastasis. Cancer Res. 2006 Mar 15;66(6):2923-7.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 496.6 |
| Cas No. | 81496-19-7 |
| Formula | C29H34NO5·1/2Ca |
| Solubility | ≤5mg/ml in DMSO |
| Chemical Name | (4Z)-rel-7-[(1R,2R,5S)-5-([1,1'-biphenyl]-4-ylmethoxy)-2-(4-morpholinyl)-3-oxocyclopentyl]-4-heptenoic acid, hemicalcium salt |
| SDF | Download SDF |
| Canonical SMILES | O=C1C[C@H](OCC2=CC=C(C3=CC=CC=C3)C=C2)[C@H](CC/C=C\CCC([O-])=O)[C@H]1N4CCOCC4.O=C5C[C@H](OCC6=CC=C(C7=CC=CC=C7)C=C6)[C@H](CC/C=C\CCC([O-])=O)[C@H]5N8CCOCC8.[Ca+2] |
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