p2yreceptor

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

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

PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.

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

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).

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

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

Uridine 5′-diphosphoglucose disodium salt (UDP-Glucose sodium salt) is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It is an agonist of the P2Y14 receptor (EC50 = 0.35 μM) and can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.

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.

YM-254890, a macrocyclohexapeptide isolated from Chromobacterium sp, is a selective and potent inhibitor of Gαq/11 protein, inhibits ADP-induced platelet aggregation and inhibits G protein signaling.

PIT (2,2'-Pyridylisatogen tosylate) is a specific, non-competitive antagonist of the Purinergic receptor P2Y1, exhibiting an IC50 of 0.14 μM for human P2Y1. It does not affect nucleotide binding and is useful in studies related to chronic bronchitis and asthma.

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.

BPTU (BMS-646786) is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

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.

MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.

NF546 (hydrate), a selective non-nucleotide P2Y11 agonist, exhibits a pEC50 value of 6.27 and induces interleukin-8 secretion from human monocyte-derived dendritic cells [1].

PSB-1114 triethylamine is a potent, enzymatically stable, P2Y2 receptor agonist with a 134 nM EC50, exhibiting greater than 50-fold selectivity over P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors [1].

Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [1].

4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4. It is utilized in crosslinking experiments and labeling of transcriptional complexes [1] [2].

4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetrasodium functions as a potent agonist at P2Y 2 and P2Y 4 receptors, with half-maximal effective concentrations (EC50s) of 35 nM for hP2Y 2 and 350 nM for hP2Y 4. This compound is applicable in studies involving crosslinking experiments and labeling of the transcriptional complex [1] [2].

ATP-γ-S tetrasodium (Adenosine-5'-O-(3-thiotriphosphate) tetrasodium) is a purinergic P2Y11 receptor agonist and ATP analog that induces inositol phosphate accumulation, induces insulin secretion from MIN6 pancreatic islet β-cells, and induces an increase in intracellular calcium concentration. ATP-γ-S tetrasodium inhibits the induction of the Junin virus. Junin virus-induced increase in the level of mRNA encoding bone morphogenetic protein 6 (BMP6) reduces particle-forming units (PFUs) in Junin virus-infected primary rat osteoblasts.

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