2. Signaling Pathways
  3. GPCR/G Protein
  4. P2Y Receptor

P2Y Receptor

P2Y Receptor

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P2Y receptors are a class of G protein-coupled receptors (GPCRs) activated by extracellular nucleotides (ATP, UTP, and UDP). There are eight mammalian P2Y receptor subtypes (P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14). The P2Y receptors are expressed in various cell types and play important roles in physiology and pathophysiology including inflammatory responses and neuropathic pain.

The P2Y family can be further divided into a subfamily of five P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs (“P2Y1-like”) that stimulate phospholipase C (PLC) through Gq protein and a second subfamily of P2Y12, P2Y13, and P2Y14Rs (“P2Y12-like”) that inhibit adenylate cyclase through Gi protein. Other effector pathways have been documented, such as coupling of the P2Y11R to Gs as well as to Gq in some cells to induce stimulation of cyclic AMP production.

P2Y Receptor Isoform Specific Products:

P2Y Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15876R
    Clopidogrel thiolactone (Standard)
    		Inhibitor
    Cyhalofop (Standard) is the analytical standard of Cyhalofop. This product is intended for research and analytical applications. Cyhalofop (Cyhalofop acid), the primary metabolite of Cyhalofop-butyl (HY-B0861) in susceptible grasses, is the herbicidally active metabolite. Cyhalofop-butyl is an aryloxyphenoxypropionate post-emergence herbicide widely used around the world in agriculture.
    Clopidogrel thiolactone (Standard)
  • HY-110092A
    PSB-1114 triethylamine
    		Agonist
    PSB-1114 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors.
    PSB-1114 triethylamine
  • HY-173407
    P2Y14R antagonist 4
    		Antagonist
    P2Y14R antagonist 4 (Compound 25l) is an orally active P2Y14R antagonist (IC50: 5.6 nM) with superior binding affinity to P2Y14R over PPTN. P2Y14R antagonist 4 has anti-inflammatory activity and reduces LPS (HY-D1056)-induced proinflammatory cytokines (IL-1β, IL-6, and TNF-α) release.
    P2Y14R antagonist 4
  • HY-117572
    MRS2567
    		Antagonist
    MRS2567 is a P2Y receptor antagonist with the activity of inhibiting contraction of mouse mesenteric arteries. MRS2567 can inhibit the sustained contraction caused by UTP and UDP, and inhibit the Na+, K+, 2Cl- co-transport-dependent signaling pathway, thereby affecting the myogenic tone of mouse mesenteric arteries.
    MRS2567
  • HY-137608A
    Uridine 5'-O-thiodiphosphate trisodium
    		Agonist
    Uridine 5'-O-thiodiphosphate (trisodium) (UDP-β-S (trisodium)) is a purinergic P2Y6 receptor agonist. Uridine 5'-O-thiodiphosphate (trisodium) selectively induces accumulation of inositol phosphates in 1321N1 cells expressing P2Y6 receptors (EC50 = 28 nM). Uridine 5'-O-thiodiphosphate (trisodium) induces DNA synthesis in rat aortic smooth muscle cells.
    Uridine 5'-O-thiodiphosphate trisodium
  • HY-108657
    MRS2279
    		Antagonist
    MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05).
    MRS2279
  • HY-154840A
    4-Thiouridine 5′-triphosphate tetrasodium
    		Agonist
    4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetrasodium is a potent P2Y2 and P2Y4 receptor agonist, with EC50s of 35 and 350 nM for hP2Y2 and hP2Y4, respectively. 4-Thiouridine 5′-triphosphate tetrasodium can be used in the study of crosslinking experiments, labeling of transcriptional complex.
    4-Thiouridine 5′-triphosphate tetrasodium
  • HY-174126
    P2Y1 antagonist 2
    		Antagonist
    P2Y1 antagonist 2 (Compound 19) is a P2Y1 receptor antagonist (IC50: 0.49 μM). P2Y1 antagonist 2 has significant antiplatelet aggregation activity and exerts its effects by inhibiting P2Y1 receptor. P2Y1 antagonist 2 can upregulate nuclear Nrf2 protein levels, exhibit neuroprotective effects, and resist oxidative stress damage. P2Y1 antagonist 2 can effectively reduce cerebral infarction area and improve neurobehavioral function, and can be used in the study of ischemic stroke.
    P2Y1 antagonist 2
  • HY-122048
    AR-C67085
    		Antagonist
    AR-C67085 (PSB 0413; FPL 67085) is a potent platelet P2T receptor antagonist with an pIC50 value of 8.60. AR-C67085 inhibits ADP-induced platelet aggregation.
    AR-C67085
  • HY-176739
    P2Y14R antagonist 5
    		Antagonist
    P2Y14R antagonist 5 (Compound A) is a novel P2Y14R antagonist based on a benzisoxazole skeleton (IC50: 23.60 nM, KD: 7.26 μM). P2Y14R antagonist 5 reduces the levels of proinflammatory cytokines (IL-1β, IL-6, TNF-α) and myeloperoxidase (MPO). P2Y14R antagonist 5 has anti-inflammatory activity in a mouse model of LPS-induced acute lung injury.
    P2Y14R antagonist 5
  • HY-174127
    P2Y1 antagonist 3
    		Antagonist
    P2Y1 antagonist 3 (compound 36b) is a blood-brain barrier (BBB)-penetrant P2Y1 antagonist with an IC50 of 0.50 μM. P2Y1 antagonist 3 exhibits protective effects in a rat middle cerebral artery occlusion (MCAO) model and demonstrates neuroprotective activity against oxidative stress by upregulating nuclear Nrf2 protein levels.
    P2Y1 antagonist 3
  • HY-113359AS3
    Uridine 5'-diphosphate-15N2 dilithium
    		Agonist
    Uridine 5'-diphosphate-15N2 dilithium is 15N labeled Uridine 5'-diphosphate (HY-113359). Uridine 5'-diphosphate is a P2Y6 receptor agonist with an EC50 of 0.013 μM for human P2Y6 receptor.
    Uridine 5'-diphosphate-<sup>15</sup>N<sub>2</sub> dilithium
  • HY-110092
    PSB-1114 tetrasodium
    		Agonist
    PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors.
    PSB-1114 tetrasodium
  • HY-136501
    MRS2395
    		Antagonist
    MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.
    MRS2395
  • HY-146498
    Antiplatelet agent 1
    		Inhibitor
    Antiplatelet agent 1 (compound 7q) is a Ticagrelor analoguehas, possessing antiplatelet activity. Antiplatelet agent 1 can be used for researching platelet aggregation.
    Antiplatelet agent 1
  • HY-108663
    5-OMe-UDP
    		Agonist
    5-OMe-UDP (5-methoxyuridine 5'-trihydrogen diphosphate) is a P2Y6 receptor agonist (EC50=0.08 μM). 5-OMe-UDP activates the P2Y6 receptor by binding to it, which triggers signaling pathways within the cell. This activation can lead to an increase in intracellular calcium ion concentration, which in turn regulates cellular function. The methoxy groups of 5-OMe-UDP provide additional activity and selectivity, contributing to the binding of 5-OMe-UDP to the P2Y6 receptor. 5-OMe-UDP can be used to study diseases related to P2Y6 receptor function, such as diabetes, inflammatory bowel disease, Alzheimer's disease, etc.
    5-OMe-UDP
  • HY-137603
    Uridine-5'-O-3-thiotriphosphate
    		Agonist
    Uridine-5'-O-(3-thiotriphosphate) (UTPγS), a stable analogue of UTP, is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability.
    Uridine-5'-O-3-thiotriphosphate
  • HY-17459S
    Clopidogrel-d3 hydrogen sulfate
    Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor.
    Clopidogrel-d<sub>3</sub> hydrogen sulfate
  • HY-117356B
    MRS2693 trisodium
    		Agonist
    MRS2693 trisodium is a selective P2Y6 agonist with an EC50 value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model.
    MRS2693 trisodium
  • HY-123490
    Regrelor disodium
    		Antagonist
    Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research.
    Regrelor disodium
Cat. No. Product Name / Synonyms Application Reactivity
P2Y Receptor Isoform Comparison

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