AH 6809

Names

[ Name ]:
AH 6809

[Synonym ]:
6-Isopropoxy-9-oxo-9H-xanthene-2-carboxylic acid
Tocris-0671
9H-Xanthene-2-carboxylic acid, 6-(1-methylethoxy)-9-oxo-
AH 6809
6-Isopropoxy-9-oxoxanthene-2-carboxylic acid

Biological Activity

[Description]:

AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.IC50 Value: ~3 nM (EC50 for calcium mobilization by PGE2) [1]Target: EP/DP receptorin vitro: AH6809also antagonized the aggregatory effect of U-46619 in whole blood (pA2 = 4.45). However, concentrations of AH6809 up to 300 microM were without effect upon either ADP- or platelet activating factor (Paf)-induced aggregation (pA2 less than 3.5) [2]. Preincubation of control cells in 10(-4) M concentrations of AH6809 inhibited PGE2-induced activation of AC by greater than 80% without significant (P greater than .05) inhibition of basal activity by the antagonist [3].in vivo: Exposure to a selective COX-2 inhibitor (SC58125) or an EP1/EP2 antagonist (AH6809), but not an EP4 antagonist (AH23848B), significantly reduced cell proliferation of esophageal explants in 24 hour-organ culture experiments [4]. Oral administration of the EP1 receptor antagonist, AH6809 (10 mg/kg/day, for 4 days), significantly reduced the systolic blood pressure in db/db, but not in control mice [5].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Inflammation/Immunology

[References]

[1]. http://www.millipore.com/publications.nsf/a73664f9f981af8c852569b9005b4eee/cae2c825891fb78e85257b19005fa865/$FILE/HTS099C%20ep1%20datasheet%20121212.pdf

[2]. Keery RJ, et al. AH6809, a prostaglandin DP-receptor blocking drug on human platelets. Br J Pharmacol. 1988 Jul;94(3):745-54.

[3]. Capehart AA, et al. Effects of a putative prostaglandin E2 antagonist, AH6809, on chondrogenesis in serum-free cultures of chick limb mesenchyme. J Cell Physiol. 1991 Jun;147(3):403-11.

[4]. Piazuelo E, et al. Characterization of the prostaglandin E2 pathway in a rat model of esophageal adenocarcinoma. Curr Cancer Drug Targets. 2012 Feb;12(2):132-43.

[5]. Rutkai I, et al. Activation of prostaglandin E2 EP1 receptor increases arteriolar tone and blood pressure in mice with type 2 diabetes. Cardiovasc Res. 2009 Jul 1;83(1):148-54.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
514.2±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₄O₅

[ Molecular Weight ]:
298.290

[ Flash Point ]:
192.9±23.6 °C

[ Exact Mass ]:
298.084137

[ PSA ]:
76.74000

[ LogP ]:
3.91

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.618

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

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