AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders.
性状
Solid
IC50 & Target[1][2]
P2Y12 Receptor
11 nM (IC50)
体外研究(In Vitro)
AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM.
AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively.
AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AZD1283 exhibits poor liver microsomal stability in rat (T1/2 = 6.08 min), but better in dog microsomes (T1/2 = 201 min) and human microsomes (T1/2 = 65.0 min).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Sprague-Dawley rats
Dosage:
5 mg/kg
Administration:
p.o.; single dosage
Result:
Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.