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.
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- CAS No.: 65425-48-1
- 화학식: C11H11NO4
- 분자량:221.21
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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 (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.
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Animal Model:Charles River rats (180-200 g)[2]
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Dosage:0.01-0.3 mg/kg (i.p.); 30-300 mg/kg (oral)
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Administration:i.p. (15-30 seconds before antigen challenge); oral (5 minutes before antigen challenge)
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Result:Inhibited histamine release from sensitized peritoneal mast cells in a dose-dependent manner via both intraperitoneal and oral routes.
Required approximately 100 times more oral dose to achieve comparable inhibition to intraperitoneal administration.
Nonspecific histamine release was 2.2%.
Chemical Information
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CAS No. 65425-48-1
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분자량 221.21
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화학식 C11H11NO4
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SMILES
O=C(OCC)C(=O)NC1=CC=CC=CC1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)