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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(11)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(191)

Protease-activated Receptor

Neuroscience

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(51)

iGluR

(130)

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.

Filter HomeSignaling PathwaysNeuroscience-GPCR/G ProteinP2Y Receptor

PPTN hydrochloride

T635341992047-65-0In house

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.

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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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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) and can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.

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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.

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Cited

cangrelor tetrasodium

T5036163706-36-3

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

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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.

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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).

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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.

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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.

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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.

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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.

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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.

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Clopidogrel

T0182113665-84-2

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

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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.

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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.

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PIT

T2316456583-49-4

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.

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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.

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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.

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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.

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N6-(4-Hydroxybenzyl)adenosine

T12164110505-75-4In house

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

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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, curbs cell proliferation, and reduces inflammation.

$117

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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).

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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]-) is a P2Y12 inhibitor.

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HDL-16

T865652373280-36-3

HDL-16 is a highly effective P2Y14R antagonist with anti-colitis effects, targeting P2Y14R in intestinal epithelial cells to alleviate ulcerative colitis.

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PSB-0739

T231951052087-90-7

PSB-0739 Selective platelet P2Y12 receptor antagonist characterized by competitive binding and high affinity (Ki =24.9 nM) with antithrombotic and platelet aggregation modulating effects.

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Selatogrel

T713641159500-34-1

Selatogrel (ACT-246475) is a selective and potent P2Y12 receptor antagonist with antithrombotic activity and inhibition of platelet aggregation for the study of acute myocardial infarction.

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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.

$1,199

35 days

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ATP-γ-S tetrasodium

T8382788453-52-5

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.

$398

35 days

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2-Methylthioadenosine diphosphate trisodium

T23581475193-31-8

2-Methylthioadenosine diphosphate trisodium (2-MeS-ADP) is the salt form of 2-Methylthioadenosine diphosphate, a synthetic analog of adenosine diphosphate (ADP), a potent purinergic P2Y receptor agonist that agonizes human P2Y13 at nanomolar levels, mouse P2Y13 and human P2Y12, induces platelet aggregation and morphological changes, and is indicated for neurological and cardiovascular disease studies.

$143

35 days

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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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2-Methylthio-ATP tetrasodium

T22496100020-57-3

2-Methylthio-ATP tetrasodium (2-MeS-ATP tetrasodium) is a non-specific P2 receptor agonist, which can activate P2X2 and P2Y1 receptors and mimic the physiological effects of ATP by binding to P2 receptors, and is widely used in the study of cell signaling and metabolic processes. In addition, 2-Methylthio-ATP tetrasodium induces non-competitive inhibition of ADP-induced platelet aggregation in human.

$253

35 days

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P2Y14 antagonist 1

T205734

P2Y14 antagonist 1 (compound 45) is a highly selective and orally active P2Y14 receptor antagonist with an IC50 value of 0.70 nM. It demonstrates significant anti-inflammatory effects by effectively reducing pulmonary infiltration of immune cells and inflammatory responses through the inhibition of the NLRP3 signaling pathway. P2Y14 antagonist 1 is suitable for studying acute lung injury.

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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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8-10 weeks

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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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8-10 weeks

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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 disodium

T7919768507-49-3

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].

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MRS2905 trisodium

T2046873033550-04-5

MRS2905 (α,β-Methylene-2-thio-UDP) trisodium is a selective P2Y14R agonist with an EC50 of 0.92 nM. It shows no activity on UDP-activated P2Y6 receptors or other P2Y receptors.

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10-14 weeks

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NSC380324

T205528

NSC380324 is a P2Y12 receptor antagonist with antiplatelet properties, which can be employed in research on atherosclerotic cardiovascular diseases.

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MRS4833

T2008372801627-78-9

MRS4833 (compound 15) is an orally active, potent, competitive antagonist of P2Y14R, exhibiting IC50 values of 5.92 nM for hP2Y14R and 4.8 nM for mP2Y14R. It reduces airway eosinophilia in protease-mediated asthma models and reverses chronic neuropathic pain in mouse CCI models.

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3-6 months

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P2Y6R antagonist 1

T200515

P2Y6R antagonist 1 (compound 5ab) is a selective, orally active antagonist of P2Y6R, featuring an IC50 value of 19.6 nM. This compound also exhibits anti-inflammatory properties.

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P2Y14R antagonist 3

T205281

P2Y14R antagonist 3 (compound A) is an orally active P2Y14R antagonist with an IC50 of 23.60 nM and a Kd of 7.26 μM. It mitigates lung injury in mice induced by Lipopolysaccharides (LPS) and can be utilized in the study of inflammatory diseases.

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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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