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| Cat. No. : | HY-10419 |
| M.Wt: | 477.60 |
| Formula: | C29H35NO5 |
| Purity: | >98 % |
| Solubility: |
AH23848 (compound 6) is a competitive blocker of the thromboxane A2 receptor and an orally effective agent, with an IC50 value of 50 nM against human targets and a long duration of action. AH23848 shows no activity against other prostaglandin, serotonin (5-HT) or adenosine diphosphate (ADP) receptors. AH23848 can be used in the research of occlusive vascular diseases[1].
In Vitro:AH23848 (compound 6) (3.0×10-8-3.0×10-6 mol/liter; 30 min) acts as a competitive antagonist of thromboxane A2 receptors in isolated human pulmonary artery smooth muscle with a pA2 of 7.8[1].
AH23848 (6.0×10-8-6.0×10-6 mol/liter; 1.0×10-5 mol/liter) competitively antagonizes thromboxane A2 receptors in isolated rat aorta smooth muscle with a pA2 of 7.94, and does not block 5-HT or potassium chloride-induced contractions at concentrations up to 1.0×10-5 mol/liter[1].
AH23848 (1.0×10−6 mol/liter) does not block PGE2- or PGF2α-induced contractions in isolated non-vascular smooth muscle preparations[1].
AH23848 (1.0×10-7-1.0×10-4 mol/liter) potently and specifically inhibits thromboxane receptor-dependent platelet aggregation in human platelet-rich plasma, with IC50 values ranging from 1.05×10-7 to 6.3×10-7 mol/liter for different agonists, and does not block ADP-, 5-HT-, or epinephrine-induced aggregation[1].
In Vivo:AH23848 (0.03-1.0 mg/kg; i.v.; single bolus) potently and specifically inhibits collagen-induced thromboembolic and bronchoconstrictor responses in anesthetized guinea pigs, with no effect on ADP-induced thrombocytopenia at doses up to 1.0 mg/kg i.v[1].
AH23848 (0.01-0.3 mg/kg; i.v.; single bolus) specifically antagonizes U-46619-induced mesenteric vasoconstriction in anesthetized Beagle dogs without altering baseline hemodynamic parameters, with a 6.5-fold rightward shift of the U-46619 dose-response curve at 0.1 mg/kg i.v[1].
AH23848 (1 mg/kg; p.o.; single dose) produces sustained, specific inhibition of collagen-induced platelet aggregation in conscious Beagle dogs, with peak effects showing a 23-fold rightward shift of the collagen dose-response curve and residual activity lasting at least 11 hours[1].
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