AY 25674 

AY 25674 is an orally active antiallergic agent and a PDE inhibitor. AY 25674 inhibits the release of allergic histamine from mast cells. AY 25674 suppresses passive anaphylaxis induced by reaginic (IgE) antibodies. AY 25674 does not inhibit the increased vascular permeability caused by non-reaginic antibodies, serotonin or histamine. AY 25674 reaches its peak activity shortly after administration; rapid tolerance occurs at high doses. AY 25674 can be used in research related to passive anaphylaxis^[1][2].

AY-25,674 exerts a significant inhibitory effect on the enzymatic activity of bovine heart PDE in the in vitro assay for inhibiting bovine heart cyclic 3',5'-PDE activity, with its inhibitory potency being approximately 1/3 that of theophylline^[1].
In an in vitro guinea pig lung adenylate cyclase activity assay, AY-25,674 (1×10^-4 M; 15 min) only increases the basal activity of PDE-free guinea pig lung adenylate cyclase by 7%, showing no significant direct activating effect on cyclic adenosine monophosphate (cAMP) production^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AY 25674 (1-100 mg/kg; i.v., i.p., oral; single or repeated doses) dose-dependently inhibits reagin-mediated passive paw anaphylaxis edema in rats via intravenous, intraperitoneal, and oral routes, with maximal oral activity at 5 minutes post-administration, induction of tachyphylaxis with repeated high doses, and relative potencies comparable to other oral antiallergic agents^[2].
AY 25674 (10 mg/kg; i.v.) specifically inhibits reagin-mediated increased capillary permeability in rats, with no significant effect on permeability induced by nonreaginic mechanisms or direct mediator action^[2].
AY 25674 (0.01-0.3 mg/kg i.p.; 30-300 mg/kg oral; i.p. 15-30 seconds before challenge; oral 5 minutes before challenge) dose-dependently inhibits reagin-mediated histamine release from rat peritoneal mast cells via intraperitoneal and oral routes, with lower potency observed with oral administration^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

221.21

C₁₁H₁₁NO₄

65425-48-1

O=C(OCC)C(=O)NC1=CC=CC=CC1=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pugsley T A, Lippmann W. Effects of [N-(2-oxo-3, 5, 7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3′, 5′-nucleotide formation and phosphodiesterase activity[J]. Experientia, 1979, 35(1): 88-90.

  [2]. Martel PR, et al. Inhibition of passive anaphylaxis induced in the rat hind paw and peritoneal cavity by N-(2-oxo-3,5,7-cycloheptatrien-1-yl)-aminooxoacetic acid ethyl ester (AY-25,674). Can J Physiol Pharmacol. 1978;56(6):1005-1010.  [Content Brief]