AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth[1][2].
2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1[1][2][3].
Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM). IC50 value: 6.77-141 μMTarget: P2Y12receptorAnti-aggregation activity of N6-(4-Hydroxybenzyl)adenosine could involve an interaction with the P2Y12receptor binding site.
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].
Prasugrel hydrochloride is a platelet inhibitor with IC50 value of 1.8 μM.Target: P2Y12 receptorPrasugrel hydrochloride is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI [2].Prasugrel hydrochloride reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel hydrochloride AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 Μm [2]. Clinical indications: Acute coronary syndrome; Ischemic heart disease; Sickle cell anemia; Stroke; Vascular occlusive diseaseFDA Approved Date: February 2009Toxicity: Hypertension; Headache; Hypercholesterolemia/hyperlipidemia; Nausea; Epistaxis
MRS 2179 is a potent, selective, competitive P2Y1 receptor antagonist with Kb of 100 nM; displays no appreciable activity at P2Y2, P2Y4, or P2Y6 receptors (>30 uM); inhibits ADP-induced platelet shape change, aggregation and Ca2+ rise but has no effect on ADP-induced inhibition of adenylyl cyclase; decreases platelet count in mice.
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes[1].
Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis, the substrate of carboxylesterase 2 (CES2)[1]. Vicagrel demonstrates a favorable safety profile and excellent anti-platelet activity, which could be an anti-platelet drug and for the unmet medical needs of cardiovascular diseases[2].
Denufosol tetrasodium (INS37217) is a long-acting P2Y2 receptor agonist, which exhibits an EC50 of ~10 μM for P2Y2 receptor activation[1].
2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation[1][2][3].
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects[1].
Suramin sodium salt is a polysulfonated naphthylurea with various biological activities. Suramin sodium salt is a DNA topoisomerase II inhibitor with an IC50 of 5 μM.
Ticagrelor-d7 (AZD6140-d7) is the deuterium labeled Ticagrelor. Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation[1][2].
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[1][2][3].
YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway. Thrombosis Discontinued
MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity[1][2][3].
Uridine 5′-diphosphoglucose-13C6 (disodium) is the 13C labeled Uridine 5′-diphosphoglucose disodium salt[1]. Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR[2].
Prasugrel-d4 is the deuterium labeled Prasugrel[1]. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[2].
Blue FPG-A trisodium is a selective antagonist of P2X1 receptor and P2Y1 receptor with IC50 values of 35.5 μM and 2.6 μM, respectively. Blue FPG-A trisodium is a structural isomer of the components of Reactive Blue 2 (RB2)[1].
UDP-Galactose is a monosaccharide involved in nucleotide sugar metabolism. UDP-Galactose and its derivatives act as a natural agonist for Gi protein-conjugated P2Y14 receptors in the immune system (IC50=0.67 μM, hP2Y14)[1].
AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.IC50 value: 3.0 ug/kg/min(EC50) [1]Target: P2Y12 receptor inhibitorAZD1283 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 that induced a larger than 3-foldincrease in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 forboth compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.
PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM[1]. PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis[2].
Oral antiplatelet agent 1 is a potent antiplatelet agent with an IC50 of 2.94 μM in vitro as well as antithrombotic efficacy in a rat model. P2Y receptor antagonist[1].
Antiplatelet agent 2 (compound 7p) is a Ticagrelor analoguehas, possessing antiplatelet activity. Antiplatelet agent 2 can be used for researching platelet aggregation[1].
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist[1][2].
Prasugrel is a platelet inhibitor with IC50 value of 1.8 μM.IC50 value:Target: P2Y12 receptorPrasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI. Prasugrel reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 μm. From Wikipedia
Prasugrel Maleic acid is a platelet inhibitor with IC50 value of 1.8 μM.Target: P2Y12 receptorPrasugrel Maleic acid is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI [2].Prasugrel Maleic acid reduces the aggregation ("clumping") of platelets by irreversibly binding to P2Y12 receptors. In rat platelets, prasugrel Maleic acid AM inhibited in vitro platelet aggregation induced by ADP (10 μm) with an IC50 value of 1.8 Μm [2]. Clinical indications: Acute coronary syndrome; Ischemic heart disease; Sickle cell anemia; Stroke; Vascular occlusive diseaseFDA Approved Date: February 2009Toxicity: Hypertension; Headache; Hypercholesterolemia/hyperlipidemia; Nausea; Epistaxis