p2y2 receptor

MRS2698 is an effective and highly selective agonist of the P2Y2 receptor (EC50: 8 nM). MRS2698 also is >300-fold P2Y2-selective versus the P2Y4 and P2Y6 receptors.

PSB-1114 tetrasodium shows >50-fold selectivity versus the P2Y4 (EC50: 9.3 μM) and P2Y6 (EC50: 7.0 μM) receptors. PSB-1114 tetrasodium is an effective, enzymatically stable, and subtype-selective P2Y2 receptor agonist (EC50: 134 nM) .

Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.

2-Thio-UTP is a selective P2Y2 receptor (purinergic receptor) agonist (EC50 = 50 nM) capable of inhibiting calcification potential, α-smooth muscle actin expression, and pro-fibrotic gene expression in valvular interstitial cells (VICs). It may be employed in studies of calcific aortic valve stenosis (CAVS).

4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4. It is utilized in crosslinking experiments and labeling of transcriptional complexes [1] [2].

4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetrasodium functions as a potent agonist at P2Y 2 and P2Y 4 receptors, with half-maximal effective concentrations (EC50s) of 35 nM for hP2Y 2 and 350 nM for hP2Y 4. This compound is applicable in studies involving crosslinking experiments and labeling of the transcriptional complex [1] [2].

PPTN is a high-affinity, competitive and highly selective antagonist of P2Y14 receptor(KB value of 434 pM), with anti-inflammatory and immune activity.

PPTN hydrochloride is a potent, high-affinity, competitive, and highly selective P2Y14 receptor antagonist (KB: 434 pM) with no agonist or antagonist activity at P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors, exhibiting anti-inflammatory and anti-immune effects.

Uridine triphosphate (UTP) is a purine nucleotide P2U receptor agonist with potential use in lung cancer treatment. By activating P2Y2 receptors, it enhances the proliferation of human cancerous ductal epithelial cells. Additionally, UTP induces fibrotic responses in cardiac fibroblasts through P2Y2 receptor activation and prolongs the action potential duration of guinea pig papillary muscles via the P2Y2 purinergic receptor.

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

PSB 1114 is an effective and selective agonist of the P2Y2 receptor (EC50: 0.134 μM).

P2Y2 and P2Y4 receptor agonist

MRS2179 is a competitive P2Y1 receptor antagonist with a Kb value of 100 nM and exhibits no appreciable activity at P2Y2, P2Y4, or P2Y6 receptors at concentrations up to 30 µM, nor at P2Y12 and P2Y13 receptors. MRS2179 inhibits ADP-induced platelet shape change and platelet aggregation in vitro, with a pA2 value of 6.55, and prolongs bleeding time in rats and mice relative to control groups. The receptor selectivity profile of MRS2179 supports its application in research focused on purinergic signaling, platelet biology, thrombosis-related mechanisms, and P2Y1 receptor-mediated cellular responses.

AR-C126313 is a selective P2Y2 receptor antagonist that inhibits ATP-mediated signaling pathways. In cell and animal models, AR-C126313 can modulate inflammation-related signaling, such as IL-6 production and p38 MAPK phosphorylation, and has been used to study fibrosis and tumor-related processes under specific experimental conditions.

MRS2578, an effective P2Y6 receptor antagonist with IC50 of 37 nM, shows insignificant inhibition at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

MRS2179 tetrasodium hydrate, a competitive antagonist of the P2Y1 receptor, acts on the turkey P2Y1 receptor (Kb: 102 nM, pA2: 6.99) and exhibits an inhibitory effect on platelet aggregation. IC50: 1.15 μM), P2X3 (IC50: 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors.

MRS2768 tetrasodium salt, a moderately potent and selective agonist of the P2Y2 receptor, exhibits a protective effect against ischemic damage in cardiomyocytes both in vivo and in vitro.

Uridine triphosphate (Uridine 5'-triphosphate) increases proliferation of human cancerous pancreatic duct epithelial cells by activating P2Y2 receptor.

PSB-1114 triethylamine is a potent, enzymatically stable, P2Y2 receptor agonist with a 134 nM EC50, exhibiting greater than 50-fold selectivity over P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors [1].

UDP-β-S, serving as a specific agonist for the purinergic P2Y6 receptor, effectively promotes inositol phosphate accumulation in 1321N1 cells containing P2Y6 receptors, with an EC50 value of 28 nM. This selectivity is evident when compared to its effects on cells expressing P2Y1, P2Y2, or P2Y4 receptors, where a concentration of 10 µM is used. Additionally, at a concentration of 1 µM, UDP-β-S stimulates DNA synthesis in isolated rat aorta smooth muscle cells.

Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) (Rp-dUTP-α-S), a sulfur-containing nucleotide isomer and purinergic P2Y2 receptor agonist, preferentially promotes inositol phosphate accumulation in 1321N1 astrocytoma cells with P2Y2 receptors (EC50 = 12.5 µM) compared to those expressing P2Y4 receptors at a concentration of 10 µM.

Uridine-5'-O-(3-thiotriphosphate) (UTP-γ-S) is a hydrolysis-resistant UTP derivative and an agonist of the purinergic P2Y2 receptor. It effectively induces inositol phosphate formation in 1321N1 astrocytoma cells harboring the human P2Y2 receptor (EC50 = 240 nM) and stimulates chloride secretion in a dose-dependent manner in primary nasal epithelial cells from cystic fibrosis patients. Moreover, UTP-γ-S prompts vasoconstriction in isolated human coronary arteries (EC50 = 25.1 µM).

Uridine adenosine tetraphosphate (UP4A) acts primarily as an endothelium-derived vasoconstrictor, exerting its effects mainly through the P2X1 receptor, and potentially through the P2Y2 and P2Y4 receptors as well. It is utilized in research related to cardiovascular diseases.