1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. AH23848 hemicalcium salt

AH23848 hemicalcium salt is an orally active, selective competitive blocker of the thromboxane A2 receptor, with an IC50 value of 50 nM. AH23848 hemicalcium salt shows no activity against other prostaglandin, serotonin (5-HT) or adenosine diphosphate (ADP) receptors. AH23848 hemicalcium salt can be used in the research of occlusive vascular diseases.

For research use only. We do not sell to patients.

AH23848 hemicalcium salt

AH23848 hemicalcium salt Chemical Structure

CAS No. : 81496-19-7

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Description

AH23848 hemicalcium salt is an orally active, selective competitive blocker of the thromboxane A2 receptor, with an IC50 value of 50 nM. AH23848 hemicalcium salt shows no activity against other prostaglandin, serotonin (5-HT) or adenosine diphosphate (ADP) receptors. AH23848 hemicalcium salt can be used in the research of occlusive vascular diseases[1].

IC50 & Target

Thromboxane Receptor[1]

In Vitro

AH23848 (compound 6) (3.0×10-8-3.0×10-6 mol/liter; 30 min) hemicalcium salt 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) hemicalcium salt 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) hemicalcium salt 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) hemicalcium salt 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].

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

In Vivo

AH23848 (0.03-1.0 mg/kg; i.v.; single bolus) hemicalcium salt potently and specifically inhibits collagen-induced thromboembolic and bronchoconstrictor responses in anesthetized guinea pigs[1].
AH23848 (0.01-0.3 mg/kg; i.v.; single bolus) hemicalcium salt specifically antagonizes U-46619-induced mesenteric vasoconstriction in anesthetized Beagle dogs without altering baseline hemodynamic parameters[1].
AH23848 (1 mg/kg; p.o.; single dose) hemicalcium salt produces sustained, specific inhibition of collagen-induced platelet aggregation in conscious Beagle dogs[1].

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

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

496.62

Formula

C29H34NO5.1/2Ca

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([O-])CC/C=C\CC[C@@H]1[C@@H](N2CCOCC2)C(C[C@@H]1OCC3=CC=C(C4=CC=CC=C4)C=C3)=O.[1/2 Ca2+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 97.0%

References
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Product Name:
AH23848 hemicalcium salt
Cat. No.:
HY-10419A
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