P2Y1 Receptor Antagonist

BPTU (BMS-646786) is a non-nucleotide P2Y₁ receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.

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.

P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC₅₀ of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis.

Desmodilactone is a P2Y1R allosteric antagonist. Desmodilactone can be used for the research of thrombosis.

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

MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a K_b of 102 nM and a pA₂ of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC₅₀=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.

Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors.

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).

BMS-884775 is a selective and orally active P2Y1 antagonist with an IC₅₀ of 0.1 nM for the human P2Y1 receptor. BMS-884775 has a similar efficacy in preventing arterial thrombosis to Clopidogrel (HY-15283) and Prasugrel (HY-15284), but treatment with BMS-884775 results in shorter bleeding time and lower bleeding risk. BMS-884775 can be used in research related to antiplatelet and arterial thrombosis-associated diseases.

MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with K_B of 0.177 μM.

TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors (IC₅₀ = 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors). TNP-ATP reduces acetate-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors (IC₅₀ = 100 and 62 nM, respectively). TNP-ATP dose-dependently attenuates acetate-induced abdominal contractions in a mouse visceral pain model (ED₅₀ = 6.35 µmol/kg)^[1][2].

P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca²⁺ increase (IC₅₀ = 1.95 μM) and platelet aggregation (IC₅₀ = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction.

P2Y1/P2Y6 antagonist 1 (Compound 3h) is an indolesulfonylhydrazide derivative. P2Y1/P2Y6 antagonist 1 is an orally active tP2Y1 and rP2Y6 antagonist (IC₅₀ of 9.72 and 1.89 μM, respectively). P2Y1/P2Y6 antagonist 1 can be used in the study of neurological diseases, inflammation, cardiovascular diseases and cancer.

Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca²⁺ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group.

MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a K_i of 2.5 nM and an IC₅₀ of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pK_B=8.05).

P2Y1 antagonist 1 (compound 10q) is a potent antagonist of P2Y1, with the IC₅₀s of 1.1 nM and 0.24 μM in FLIPR assay and hPA assay, respectively. P2Y1 antagonist 1 plays an important role in antiplatelet research.

Adenosine 3'-phosphate 5'-phosphosulfate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca²⁺ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group.

MRS2603 is a pyridoxal derivative. MRS2603 antagonized both P2Y1 and P2Y13 receptors.

MRS2496 is a selective P2Y1 receptor antagonist with an IC₅₀ value of 1.5 μM, exhibiting antiplatelet aggregation activity. MRS2496 can be used in the research of antiplatelet aggregation and blood-related diseases.

Adenosine 3'-phosphate 5'-phosphosulfate triethylamine, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca²⁺ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group.