AH6809 Inhibitor – Ah 6809

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: ~3nM (EC50 for calcium mobilization by PGE2) [1] Oral administration of the EP1 receptor antagonist, AH6809 (10mg/kg/day, for 4 days), significantly reduced the systolic blood pressure in db/db, but not in control mice [5]. 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]. Target: EP/DP receptor in vitro: AH6809also antagonized the aggregatory effect of U-46619 in whole blood (pA2 = 4.45). However, concentrations of AH6809 up to 300microM were without effect upon either ADP- or platelet activating factor (Paf)-induced aggregation (pA2 less than 3.5) [2]. 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].

http://www.millipore.com/publications.nsf/a73664f9f981af8c852569b9005b4eee/cae2c825891fb78e85257b19005fa865/FILE/HTS099C%20ep1%20datasheet%20121212.pdf
http://www.millipore.com/publications.nsf/a73664f9f981af8c852569b9005b4eee/cae2c825891fb78e85257b19005fa865/FILE/HTS099C%20ep1%20datasheet%20121212.pdf
Keery RJ, et al. AH6809, a prostaglandin DP-receptor blocking drug on human platelets. Br J Pharmacol. 1988 Jul;94(3):745-54.
Keery RJ, et al. AH6809, a prostaglandin DP-receptor blocking drug on human platelets. Br J Pharmacol. 1988 Jul;94(3):745-54.
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.
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.
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.
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.
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.
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.

Small volumes of AH6809, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5754489 is an inhibitor targeting AH6809. Also known as AH 6809.