P2Y Receptor Antagonist

Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.

P2Y1 antagonist 6 (Example 30) is a P2Y1 receptor (P2Y1 Receptor) antagonist and can be used in antithrombotic research.

Selatogrel (ACT-246475) is a reversible and selective P2Y₁₂ receptor antagonist which inhibits platelet aggregation with an IC₅₀ of 8 nM. Selatogrel exhibits antithrombotic efficacy.

MRS 2578 is a selective and potent P2Y6 receptor antagonist with IC₅₀s of 37 nM (human) and 98 nM (rat). MRS 2578 exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

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.

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.

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

PPTN, a chemical probe, is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a K_B value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity.

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.

PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a K_B value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity.

MRS2179 tetrasodium hydrate 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 hydrate is selective for P2Y1 over P2X1 (IC₅₀=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium hydrate inhibits platelet aggregation.

NF157 is a highly selective nanomolar P2Y11 antagonist with a pK_i of 7.35. The IC₅₀s are 463 nM, 1811 µM, 170 µM for P2Y11 (K_i=44.3 nM), P2Y1 (K_i=187 µM), P2Y2 (K_i=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).

MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC₅₀= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system.

MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (K_i=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.

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

AZD1283 is a potent P2Y₁₂ receptor antagonist with a binding IC₅₀ of 11 nM and a GTPγS IC₅₀ of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders.

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 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC₅₀ value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis.

P2Y6R antagonist 1 (compound 5ab) is a selective, orally active P2Y6R antagonist with an IC₅₀ value of 19.6 nM. P2Y6R antagonist 1 has anti-inflammatory activity.

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.