P2Y2 Receptor Agonist

Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a topical treatment of dry eye disease.

4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetrasodium (Compound 15) is a UTP analog and potent P2Y₂ and P2Y₄ agonist with EC₅₀ values of 35 and 350 nM for hP2Y₂ and hP2Y₄, respectively. 4-Thiouridine 5′-triphosphate tetrasodium can be used in cross-linking experiments and transcriptional complex labeling studies.

MRS2768 tetrasodium salt is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 tetrasodium salt activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 tetrasodium salt inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 tetrasodium salt activates eNOS to increase NO secretion in endothelial cells. MRS2768 tetrasodium salt drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 tetrasodium salt exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 tetrasodium salt can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

MRS2768 is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

Uridine-5'-O-(3-thiotriphosphate) (UTPγS) tetrasodium, a stable analogue of Uridine triphosphate (UTP) (HY-107372), is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability. Uridine-5'-O-(3-thiotriphosphate) tetrasodium stimulates inositol phosphate formation in human 1321N1 astrocytoma cells stably expressing the phospholipase C-coupled human P2U-purinoceptor (EC₅₀ = 240 nM).

Diquafosol (INS365 free base) is a potent P2Y2 agonist. Diquafosol nhibits apoptosis and decreases ROS generation. Diquafosol has the potential for the research of dry eye.

2-Thio-UTP is a selective P2Y₂ inhibitor with an EC₅₀ value of 50 nM. 2-Thio-UTP reduces pro-fibrotic gene expression and protein α-smooth muscle actin. 2-Thio-UTP has the potential for the research of calcific aortic valve stenosis (CAVS) .

4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetralithium (Compound 15) is a UTP analog and potent P2Y₂ and P2Y₄ agonist with EC₅₀ values of 35 and 350 nM for hP2Y₂ and hP2Y₄, respectively. 4-Thiouridine 5′-triphosphate tetralithium can be used in cross-linking experiments and transcriptional complex labeling studies.