1. Immunology/Inflammation
  2. Thrombopoietin Receptor
  3. AH23848

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.

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AH23848

AH23848 Chemical Structure

CAS No. : 81443-73-4

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Description

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].

In Vivo
Animal Model: Guinea pig (anesthetized)[1]
Dosage: 0.03 mg/kg (collagen-induced responses); 1.0 mg/kg (ADP-induced thrombocytopenia)
Administration: i.v.; single bolus
Result: Substantially reduced collagen-induced thrombocytopenia.
Almost completely abolished the collagen-induced diastolic pressor response.
Nearly eliminated collagen-induced bronchoconstriction.
Showed no inhibitory effect on ADP-induced thrombocytopenia at 1.0 mg/kg.
Animal Model: Beagle dog (anesthetized)[1]
Dosage: 0.01-0.3 mg/kg
Administration: i.v.; single bolus
Result: Had little or no effect on baseline blood pressure or mesenteric arterial blood flow.
Specifically antagonized U-46619-induced mesenteric vasoconstriction.
Produced a mean 6.5-fold rightward shift in the U-46619 dose-effect curve at 0.1 mg/kg.
Animal Model: Beagle dog (conscious)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Produced a marked inhibition of collagen-induced platelet aggregation ex vivo, with a mean peak 23-fold rightward shift of the collagen concentration-aggregation curve.
Showed a residual twofold rightward shift still evident 11 hours after dosing.
Had no inhibitory effect on ADP-induced platelet aggregation ex vivo.
Molecular Weight

477.60

Formula

C29H35NO5

CAS No.
SMILES

C(C/C=C\CCC(O)=O)[C@H]1[C@@H](C(=O)C[C@H]1OCC2=CC=C(C=C2)C3=CC=CC=C3)N4CCOCC4

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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AH23848
Cat. No.:
HY-10419
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