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TargetMol | Tags GPCR/G Protein
TargetMol | Tags Neuroscience

P2Y Receptor

P2Y receptors are a family of purinergic G protein-coupled receptors, stimulated by nucleotides such as adenosine triphosphate, adenosine diphosphate, uridine triphosphate, uridine diphosphate, and UDP-glucose.To date, 8 P2Y receptors have been cloned in humans: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13 and P2Y14. P2Y receptors are present in almost all human tissues where they exert various biological functions based on their G-protein coupling. P2Y receptors mediate responses including vasodilation, blood clotting, and immune response. Due to their ubiquity and variety in function, they are a common biological target in pharmacological development.

  • Uridine-5'-diphosphate disodium salt
    T470627821-45-0
    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.
    • $32
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  • PPTN
    T125301160271-30-6In house
    PPTN is a high-affinity, competitive and highly selective antagonist of P2Y14 receptor(KB value of 434 pM), with anti-inflammatory and immune activity.
    • $117
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  • PSB-16133 sodium
    T284632089035-40-3In house
    PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.
    • $293
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  • Regrelor disodium
    T34280676251-22-2In house
    Regrelor disodium (INS 50589) is a p2y12 receptor antagonist that prevents thrombosis, effectively inhibits vascular smooth muscle cell contraction, inhibits cell proliferation, and reduces inflammation.
    • $195
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  • SYL-4
    T836376222-65-7In house
    SYL-4 is a potential P2Y12 receptor antagonist with a Ki value of 7.35 ± 1.72 for use in synthetic dyes.
    • $882
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  • Ticagrelor metabolite M5
    T210591251765-07-7
    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).
    • $84
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  • 1-[(5-methylisoxazol-3-yl)methyl]piperazine
    T8582173850-51-6
    1-[(5-methylisoxazol-3-yl)methyl]piperazine (Piperazine, 1-[(5-methyl-3-isoxazolyl)methyl]- (9CI)) is a P2Y12 inhibitor.
    • $133
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  • Elinogrel
    T11177936500-94-6In house
    Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.
    • $54
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  • PPTN hydrochloride
    T635341992047-65-0In house
    PPTN hydrochloride is a potent, high-affinity, competitive, highly selective P2Y14 receptor antagonist (KB: 434 pM), but no agonist or antagonist activity at P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12 or P2Y13 receptors, exhibiting anti-inflammatory and anti-immune effects.
    • $41
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  • N6-(4-Hydroxybenzyl)adenosine
    T12164110505-75-4In house
    N6-(4-Hydroxybenzyl)adenosine (Para-topolin riboside) is a platelet aggregation inhibitor.
    • $40
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  • PIT
    T2316456583-49-4
    PIT (2,2'-Pyridylisatogen tosylate) is a specific and non-competitive antagonist of the Purinergic receptor P2Y1 with an IC50 of 0.14 μM for human P2Y1. PIT does not affect nucleotide binding and can be used in studies about chronic bronchitis and asthma.
    • $57
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  • Diquafosol tetrasodium
    T7423211427-08-6
    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.
    • $39
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    TargetMol | Citations Cited
  • AZD1283
    T3536919351-41-0
    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.
    • $31
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  • Uridine 5′-diphosphoglucose disodium salt
    T474328053-08-9
    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). It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.
    • $42
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  • Uridine 5'-diphosphate
    T7858358-98-0
    Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [1].
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  • 4-Thiouridine 5′-triphosphate tetralithium
    T7919620188-72-1
    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].
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  • Prasugrel
    T0230150322-43-3
    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.
    • $35
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  • Ticagrelor
    T0179274693-27-5
    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).
    • $40
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  • NF546 hydrate
    T78079
    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].
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  • 4-Thiouridine 5′-triphosphate tetrasodium
    T79197
    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 (EC 50 s) 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].
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  • (±) Clopidogrel hydrogen sulfate
    T0182L2135046-48-9
    (±) 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.
    • $50
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  • Clopidogrel hydrogen sulfate
    T0182L120202-66-6
    Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.
    • $30
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  • YM-254890
    T17273568580-02-9
    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.
    • $838
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  • Clopidogrel
    T0182113665-84-2
    Clopidogrel (SR-25990C), a P2Y12 receptor antagonist, decreases platelet aggregation.
    • $41
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  • Prasugrel Hydrochloride
    T6952389574-19-0
    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.
    • $39
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  • PSB-1114 triethylamine
    T78080
    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].
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  • MRS 2578
    T6172711019-86-2
    MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.
    • $38
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  • BPTU
    T4132870544-59-5
    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.
    • $32
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    TargetMol | Citations Cited
  • cangrelor tetrasodium
    T5036163706-36-3
    Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.
    • $39
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  • Clopidogrel thiolactone
    T55011147350-75-1
    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.
    • $173
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