p2y12

PPTN is a high-affinity, competitive and highly selective antagonist of P2Y14 receptor(KB value of 434 pM), with anti-inflammatory and immune activity.

Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.

N6-(4-Hydroxybenzyl)adenosine (Para-topolin riboside) is a platelet aggregation inhibitor.

PPTN hydrochloride is a potent, high-affinity, competitive, and highly selective P2Y14 receptor antagonist (KB: 434 pM) with no agonist or antagonist activity at P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors, exhibiting anti-inflammatory and anti-immune effects.

SYL-4 is a potential P2Y12 receptor antagonist with a Ki value of 7.35 ± 1.72 for use in synthetic dyes.

Regrelor disodium (INS 50589) is a P2Y12 receptor antagonist that prevents thrombosis, effectively inhibits vascular smooth muscle cell contraction, curbs cell proliferation, and reduces inflammation.

Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).

Prasugrel (CS-747) is a piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.

Clopidogrel (SR-25990C), a P2Y12 receptor antagonist, decreases platelet aggregation.

Prasugrel Hydrochloride (LY 640315 Hydrochloride) is a piperazine derivative and pletelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.

(±) Clopidogrel hydrogen sulfate (Iscover) , an antiplatelet agent pharmacologically and structurally analogous to ticlopidine, is used to inhibit blood clots in various conditions such as cerebrovascular disease, peripheral vascular disease, and coronary artery disease.

Vicagrel is an effective, orally active antiplatelet compound that enhances the inhibitory effect of aspirin on platelet aggregation and thrombosis in rodents by irreversibly inhibiting P2Y12 receptors and reducing metabolic inactivation. Viagrel can be used to treat blood clots in coronary artery disease, peripheral vascular disease and cerebrovascular disease.

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor's immediate effect after infusion, and the therapeutic effects can be maintained with continuous infusion.

1-[(5-methylisoxazol-3-yl)methyl]piperazine (Piperazine, 1-[(5-methyl-3-isoxazolyl)methyl]-) is a P2Y12 inhibitor.

Ticagrelor metabolite M5 (T437700) is a metabolite of Ticagrelor, the first reversible oral antagonist of P2Y12 receptor. Compared to Clopidogrel, Ticagrelor has faster and more consistent inhibition on ADP-receptors. Ticagrelor is used in the treatment of acute coronary syndromes (ACS).

BX 667 is a P2Y12 receptor antagonist. BX 667 blocks ADP-induced platelet aggregation in human, dog and rat blood with IC50 value of 97, 317 and 3000 nM respectively.

2-Methylthio-AMP diTEA (2-MeSAMP) is a selective and direct antagonist of the P2Y12 receptor, effectively inhibiting ADP-dependent platelet aggregation[1][2][3].

R-138727 is a novel P2Y12 receptor inhibitor.

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug kg min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg kg min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg kg min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

Ticagrelor-d7 is a deuterated compound of Ticagrelor. Ticagrelor has a CAS number of 274693-27-5. Ticagrelor, produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).

Prasugrel chloride impurity is an orally active antagonist of P2Y12 receptor, and inhibits ADP-induced platelet aggregation.

Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist and inhibits ADP-induced platelet aggregation. Prasugrel Maleic acid is a thienopyridine and prodrug. Prasugrel Maleic acid also inhibits platelet function.

Clopidogrel thiolactone (2-oxoclopidogrel) is a potent P2Y12 receptor inhibitor and a potent antiplatelet aggregation compound.Clopidogrel thiolactone is the active metabolic intermediate resulting from the first oxidative activation of Clopidogrel.