P2Y Receptor Antagonist

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.

Loureirin D is a selective P2Y12 receptor antagonist that penetrates the blood-brain barrier. Loureirin D inhibits the MAPK/JNK/ERK/p38 signaling pathway in microglia by acting on CD38, and inhibits ADP (HY-W010918)-induced platelet aggregation, MMP2/9-mediated tight junction disruption, and ischemia-related blood-brain barrier damage. Loureirin D protects endothelial cells from OGD-induced apoptosis. Loureirin D is used in studies of ischemic stroke and thrombosis.

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

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.

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.

Becondogrel (2-Oxoclopidogrel) is the metabolite of Clopidogrel (HY-15283). Becondogrel irreversibly inhibits P2Y12 receptor, thereby inhibiting platelet aggregation and thrombosis.

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

Sp-ATPαS tetrasodium is a thiophosphonate analogue of ATP. Sp-ATPαS tetrasodium is a competitive antagonist of the human P2Y1 receptor and can inhibit the calcium signal induced by ADP. Sp-ATPαS tetrasodium has higher metabolic stability than ATP. Sp-ATPαS tetrasodium can be used to study the binding mode of metal-nucleotide in enzymatic reactions.

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

P2Y2R antagonist 1 is a selective P2Y2R antagonist (pIC₅₀ = 7.78). P2Y2R antagonist 1 can be used for the study of Glioma.

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

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.

MRS4865 (compund 7a) is a chimera of a P2Y14 receptor antagonist and a UDP-glucose agonist that protects against neuropathic pain.

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

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.

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.

AR-C67085 (PSB 0413; FPL 67085) is a potent platelet P_2T receptor antagonist with an pIC₅₀ value of 8.60. AR-C67085 inhibits ADP-induced platelet aggregation.