| Bioactivity | AH 6809 is an antagonist of EP and DP receptor, with Kis of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptor respectively. AH 6809 has a Ki of 350 nM for mouse EP2 receptor[1][2][3]. | ||||||||||||
| Invitro | AH 6809 (1 μM; 30 min) inhibits T. serrulatus venom (TsV)-induced and PGE2-amplified IL-1β and cAMP production in macrophages[4].AH 6809 (30-300 μM) antagonizes the anti-aggregatory activity of PGD2 in whole blood, with an apparent pA2 of 5.35[5]. | ||||||||||||
| In Vivo | AH 6809 (5 mg/kg; i.p.) decreases TsV-induced mortality, PGE2 and IL-1β production and neutrophil infiltration in the lungs of mice[4]. | ||||||||||||
| Name | AH 6809 | ||||||||||||
| CAS | 33458-93-4 | ||||||||||||
| Formula | C17H14O5 | ||||||||||||
| Molar Mass | 298.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Abramovitz M, et, al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. [2]. Kiriyama M, et, al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. [3]. Woodward DF, et, al. 6-Isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist. Biochem Pharmacol. 1995 Nov 9;50(10):1731-3. [4]. Zoccal KF, et, al. Opposing roles of LTB4 and PGE2 in regulating the inflammasome-dependent scorpion venom-induced mortality. Nat Commun. 2016 Feb 23;7:10760. [5]. Keery RJ, et, al. AH6809, a prostaglandin DP-receptor blocking drug on human platelets. Br J Pharmacol. 1988 Jul;94(3):745-54. |