R-138727

R-138727, the major active metabolite of Prasugrel (HY-15284), is a highly potent and selective irreversible antagonist of the P2Y12 receptor, with an IC₅₀ of 2.5 μM. R-138727 covalently binds to the P2Y12 receptor on the platelet surface, blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 can be used to study stroke, cerebral infarction and neurological deficits. In Vitro:R-138727 (0.03-100 μM; 30 min) acts as a specific antagonist for the human P2Y₁₂ receptor expressed in CHO cells, with an IC₅₀ of 2.5 μM for inhibiting [³H]-2-MeS-ADP binding^[1].
R-138727 (0.1-10 μM; 1.5 min) potently inhibits ADP-induced aggregation in washed human platelets, with an IC₅₀ value of 0.53 μM against 10 μM ADP and 0.63 μM against 0.1 μM 2-MeS-ADP^[1].
R-138727 (0.3-30 μM; 1.5-30 min) exhibits time-dependent antiplatelet activity in human platelet-rich plasma (PRP), with its IC₅₀ value decreasing from 28 μM (1.5 min) to 1.8 μM (30 min) as the pre-incubation time increases^[1]. In Vivo:R-138727 (0.03-0.3 mg/kg; intravenous injection; single dose) exerts dose-dependent antiplatelet effects in a non-human primate model of ischemic stroke, increases the recanalization rate of the middle cerebral artery (MCA), reduces cerebral infarction volume, and improves neurological deficits^[2].