MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease.

MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.

SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis.

UTPU (trisodium) (Compound 19) is a selective P2Y6R agonist with an EC50 of 0.4 μM. UTPU (trisodium) can activate the intracellular calcium signaling pathway mediated by P2Y6. UTPU (trisodium) can be used for the research of inflammation.

Rp-dUTPαS (tetrasodium) is an isomer of the sulfur-containing nucleoride dUTP-α-S and an agonist of the purinergic P2Y2 receptor. Rp-dUTPαS (tetrasodium) selectively induces inositol phosphate accumulation in P2Y2-expressing 1321N1 cells with an EC50 of 12.5 μM.

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.

Rp-UTP-α-S (tetrasodium) is a nucleotide agonist of purinergic P2Y2 and P2Y4 receptors. Rp-UTP-α-S (tetrasodium) can induce inositol phosphate accumulation in P2Y2 or P2Y4 expressing 1321N1 cells with EC50 values of 5.4 and 27 μM.

UDP trisodium (Compound 3), a nucleotide, is a P2Y14 receptor agonist with an EC50 of 160  nM for P2Y14 receptor over the P2Y6 receptor. UDP trisodium can be used for pain, diabetes, cystic fibrosis and other pulmonary diseases research.

AR-C66096 is a potent and selective antagonist of the Gi-coupled P2Y12 receptor. AR-C66096 suppresses platelet thrombus stability under physiological flow conditions. AR-C66096 inhibits ADP-induced aggregation in whole blood aggregometry. AR-C66096 can be used for antithrombotic research.

P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [18F] can be used in studies of brain PET imaging.

PSB-22219 is a highly selective non-nucleotidic ligand acting on P2Y12 receptors (KD=4.57 nM). PSB-22219 is promising for research of P2Y12 receptor-associated neuroinflammation.

NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research.

NSC380324 is a P2Y12 receptor antagonist, possessing antiplatelet activity, and can be utilized in research on atherosclerotic cardiovascular diseases.

MRS2905 (α,β-Methylene-2-thio-UDP) trisodium is a selective P2Y14R agonist with an EC50 of 0.92 nM. MRS2905 trisodium is inactive at the UDP-activated P2Y6 receptor, and at other P2Y receptors.

Becondogrel (2-Oxoclopidogrel) is the metabolite of Clopidogrel, a dihydroorotate dehydrogenase (DHODH) inhibitor with antiviral activity.

MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM).

MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R).

Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.

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 aggrega

MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05.

PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.

trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel. Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.

PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM. PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis.

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.

MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.

BPTU is an Allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM).

PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect.

2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.

MRS2768 tetrasodium salt is a moderately potent and selective P2Y2 receptor agonist. MRS2768 tetrasodium salt has a protective effect on cardiomyocytes from ischemic damage in vivo and in vitro.

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).