P2Y12 Receptor
The P2Y12 receptor is an ADP-activated platelet receptor that plays a central role in platelet activation, thrombus formation, hemostasis, and thrombosis[1][2]. Mechanistically, P2Y12 signaling amplifies platelet activation by supporting αIIbβ3 integrin activation and platelet aggregation through a phosphoinositide 3-kinase-dependent pathway[3]. In thrombin-stimulated platelets, autocrine or added ADP stimulates P2Y12 receptors to enhance and prolong Ca2+ mobilization, with PI3Kβ, rather than PI3Kγ, driving prolonged Ca2+ response, procoagulant activity, and coagulation[4]. In disease-related settings, P2Y12 inhibition supports antithrombotic therapy in coronary artery disease, acute coronary syndrome, myocardial infarction, and percutaneous coronary intervention[5][6]. Compared with related platelet activation pathways, P2Y12 can generate P2Y1-independent inside-out signaling, while PAR-1 and PAR-4 platelet responsiveness may persist despite adequate P2Y12 inhibition[3][7]. For experimental and translational applications, clopidogrel, prasugrel, ticagrelor, cangrelor, and novel reversible antagonists provide tools to study ADP-induced platelet aggregation, receptor specificity, pharmacodynamic variability, and thrombotic disease models[5][8][9].
References:
- [1]. Kim S, et al. P2Y12 receptor in platelet activation. Platelets. 2011;22(1):56-60. [Content Brief]
- [2]. Dorsam RT, et al. Central role of the P2Y12 receptor in platelet activation. J Clin Invest. 2004 Feb;113(3):340-5. [Content Brief]
- [3]. Kauffenstein G, et al. The P2Y(12) receptor induces platelet aggregation through weak activation of the alpha(IIb)beta(3) integrin--a phosphoinositide 3-kinase-dependent mechanism. FEBS Lett. 2001 Sep 14;505(2):281-90. [Content Brief]
- [4]. van der Meijden PE, et al. Dual P2Y 12 receptor signaling in thrombin-stimulated platelets--involvement of phosphoinositide 3-kinase beta but not gamma isoform in Ca2+ mobilization and procoagulant activity. FEBS J. 2008 Jan;275(2):371-85. [Content Brief]
- [5]. Vivas D, et al. Platelet P2Y₁₂ receptor inhibition: an update on clinical drug development. Am J Cardiovasc Drugs. 2010;10(4):217-26. [Content Brief]
- [6]. Kunadian V, et al. Aspirin, Platelet P2Y12 Receptor Inhibitors, and Other Oral Antiplatelets: Comparative Pharmacology and Role in Elective PCI. Interv Cardiol Clin. 2013 Oct;2(4):527-535. [Content Brief]
- [7]. Badr Eslam R, et al. Residual platelet activation through protease-activated receptors (PAR)-1 and -4 in patients on P2Y12 inhibitors. Int J Cardiol. 2013 Sep 20;168(1):403-6. [Content Brief]
- [8]. Hasegawa M, et al. Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor. Thromb Haemost. 2005 Sep;94(3):593-8. [Content Brief]
- [9]. Bryant J, et al. Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (I): in vitro effects on platelets. Thromb Res. 2008;122(4):523-32. [Content Brief]
-
P2Y12 Receptor Related Products (34)
Related Products (34)
- 1
- 2
-
2-Methylthio-AMP diTEA
0 ImagesCat. No.: HY-125989BCAS No.: 1227193-98-7Synonyms: 2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.
-
P2Y12 antagonist 2
0 ImagesCat. No.: HY-111755CAS No.: 2299200-91-0P2Y12 antagonist 2 is a potent P2Y12 receptor antagonist. P2Y12 antagonist 2 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. P2Y12 antagonist 2 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. P2Y12 antagonist 2 can be used to research thromboembolic disorders.
-
Cangrelor
0 ImagesCat. No.: HY-19638CAS No.: 163706-06-7Synonyms: AR-C69931MXCangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist.
-
SAR216471 hydrochloride
0 ImagesCat. No.: HY-110265CAS No.: 1279829-64-9SAR216471 hydrochloride is a P2Y12 receptor antagonist. SAR216471 hydrochloride has antiplatelet and antithrombotic activities in vivo.
-
Selatogrel hydrochloride
0 ImagesCat. No.: HY-109122ACAS No.: 2210298-04-5Synonyms: ACT-246475 hydrochlorideSelatogrel (ACT-246475) is a reversible and selective P2Y12 receptor antagonist which inhibits platelet aggregation with an IC50 of 8 nM. Selatogrel exhibits antithrombotic efficacy.
-
2-MeSADP
0 ImagesCat. No.: HY-108648ACAS No.: 34983-48-7Synonyms: 2-Methylthioadenosine diphosphate; 2-Methylthio-ADP2-MeSADP is a P2Y receptor agonist, with an EC50 of 5 nM for human P2Y12, EC50 values of 19 nM and 13 nM for human P2Y13, and an EC50 of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma.
-
Evategrel
0 ImagesCat. No.: HY-159839CAS No.: 2760609-74-1Synonyms: CG-0255Evategrel is a platelet aggregation inhibitor.
-
Prasugrel-d5
0 ImagesCat. No.: HY-15284SCAS No.: 1127252-92-9Synonyms: PCR 4099-d5Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
-
ACT-281959
0 ImagesCat. No.: HY-119085CAS No.: 1159501-31-1ACT-281959 is an orally active prodrug of Selatogrel (HY-109122), a P2Y12 receptor antagonist. ACT-281959 can inhibit platelet aggregation and can be used for the research of cardiovascular disease.
-
(Rac)-BX 048
0 ImagesCat. No.: HY-W419570CAS No.: 478005-11-7(Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM).
-
Elinogrel (Standard)
0 ImagesCat. No.: HY-11021RCAS No.: 936500-94-6Synonyms: PRT060128 (Standard)Elinogrel (Standard) (PRT060128 (Standard)) is the analytical standard of Elinogrel (HY-11021). This product is intended for research and analytical applications. Elinogrel (PRT060128) is an orally active, selective, competitive, and reversible direct-acting platelet P2Y12 antagonist (IC50 = 20 nM). Elinogrel blocks ADP-induced signaling by directly and reversibly competing for binding to the platelet P2Y12 receptor. Elinogrel exhibits rapid and potent anti-platelet aggregation and antithrombotic activities. Elinogrel is suitable for research into acute coronary syndrome and antithrombotic.
-
Prasugrel (Maleic acid)
0 ImagesCat. No.: HY-15284BCAS No.: 389574-20-3Synonyms: PCR 4099 (Maleic acid)Prasugrel (PCR 4099) Maleic acid is a thienopyridine and proagent, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
-
Elinogrel potassium
0 ImagesCat. No.: HY-14486CAS No.: 936501-01-8Synonyms: PRT060128 potassiumElinogrel (PRT060128) potassium is an orally active, selective, competitive, and reversible direct-acting platelet P2Y12 antagonist (IC50 = 20 nM). Elinogrel potassium blocks ADP-induced signaling by directly and reversibly competing for binding to the platelet P2Y12 receptor. Elinogrel potassium exhibits rapid and potent anti-platelet aggregation and antithrombotic activities. Elinogrel potassium is suitable for research into acute coronary syndrome and antithrombotic.
- 1
- 2
