P2Y Receptor Agonist

UTPU trisodium (Compound 19) is a selective P2Y6R agonist with an EC₅₀ of 0.4 μM. UTPU trisodium can activate the intracellular calcium signaling pathway mediated by P2Y6. UTPU trisodium can be used for the research of inflammation.

MRS2957 is a P2Y6 receptor agonist that activates AMPK in pancreatic β-cells, promoting insulin secretion and reducing apoptosis, thereby holding potential as a therapeutic target for type 2 diabetes.

UDP-Galactose is a monosaccharide and a key glycosyl donor molecule in cells that participates in nucleotide sugar metabolism. UDP-Galactose is the natural agonist of the P2Y₁₄ receptor coupled to G_i proteins in the immune system (IC₅₀ = 0.67 μM, hP2Y₁₄). UDP-Galactose can be used to study cell signal transduction and substance metabolism.

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.

mrs 4062 (TEA) is a selective P2Y₄ receptor agonist with an EC₅₀ of 23 nM. mrs 4062 (TEA) has EC₅₀s of 640 nM and 740 nM for P2Y₂ and P2Y₆, respectively.

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

Uridine 5'-diphosphate-¹³C₉ (UDP-13C9 ) dilithium is ¹³C-labeled Uridine 5'-diphosphate (HY-113359). Uridine 5'-diphosphate is a P2Y₆ receptor agonist with an EC₅₀ of 0.013 μM for human P2Y₆ receptor.

Uridine-5'-diphosphate (UDP) is an important nucleotide made of uracil, ribose, and a pyrophosphate group. Uridine-5'-diphosphate is a potent, selective human P2Y₆ receptor native agonist (EC₅₀ = 300 nM; pEC₅₀ = 6.52). Uridine-5'-diphosphate disodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis.

MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease.

2-MeSADP is a P2Y receptor agonist, with an EC₅₀ of 5 nM for human P2Y12, EC₅₀ values of 19 nM and 13 nM for human P2Y13, and an EC₅₀ of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma.

Rp-UTP-α-S (Rp-Uridine 5'-O-(1-thiotriphosphate)) tetrasodium is a nucleotide agonist of purinergic P2Y₂ and P2Y₄ receptors. Rp-UTP-α-S (tetrasodium) can induce inositol phosphate accumulation in P2Y₂ or P2Y₄ expressing 1321N1 cells with EC₅₀ values of 5.4 and 27 μM.

PSB 0474 (3-phenacyl-UDP) is a UDP (HY-113359) analog and selective P2Y₆ receptor agonist, with an EC₅₀ value of 70 nM for the hP2Y₆ receptor. PSB 0474 activates Phospholipase C-coupled receptors to increase intracellular inositol phosphate levels. PSB 0474 enhances NO release by upregulating inducible iNOS and induces Apoptosis. PSB 0474 increases micturition frequency in urine of anesthetized rats, without altering bladder contraction amplitude/duration or causing urothelial damage. PSB 0474 can be used in studies related to chronic brain inflammation.

MRS2693 ammonium is a selective P2Y6 receptor agonist. MRS2693 ammonium exerts biological effects by activating the Gq-coupled P2Y6 receptor, the ERK1/2 pathway, and the P2RY6-PLCB3-CAMKK2-PRKAA1-ULK1 signaling cascade. MRS2693 ammonium attenuates TNFα-induced NF-κB activation, stabilizes XIAP via AKT-mediated phosphorylation, induces autophagy, and reactivates PRKAA1. MRS2693 ammonium can be used in research on diseases including skeletal muscle ischemia/reperfusion injury, TNFα-induced skeletal muscle apoptosis, chronic myelomonocytic leukemia, colorectal cancer, and dry eye disease.

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.

Uridine 5'-O-thiodiphosphate trisodium (UDP-β-S trisodium) is a P2Y₆ receptor agonist with an EC₅₀ of 25 nM. Uridine 5'-O-thiodiphosphate trisodium resists degradation by extracellular nucleotidases and stimulates the accumulation of inositol phosphates. Uridine 5'-O-thiodiphosphate trisodium stimulates contractile responses in endothelium-denuded rat mesenteric arteries. As a mitogen, Uridine 5'-O-thiodiphosphate trisodium stimulates DNA synthesis, [³H] thymidine incorporation, protein synthesis, [³H]leucine incorporation, and increases the number of vascular smooth muscle cells. Uridine 5'-O-thiodiphosphate trisodium can be used in the research of cardiovascular diseases such as atherosclerosis.

UMP-CP trisodium (Compound 3), a nucleotide, is a P2Y₁₄ receptor agonist with an EC₅₀ of 160  nM for P2Y₁₄ receptor over the P2Y₆ receptor. UDP trisodium can be used for pain, diabetes, cystic fibrosis and other pulmonary diseases research.

Uridine 5'-diphosphate-¹⁵N₂ (UDP-¹⁵N₂) dilithium is the ¹⁵N₂-labeled Uridine 5'-diphosphate (HY-113359). Uridine-5'-diphosphate is an important nucleotide made of uracil, ribose, and a pyrophosphate group. Uridine-5'-diphosphate is a potent, selective human P2Y₆ receptor native agonist (EC₅₀ = 300 nM; pEC₅₀ = 6.52). Uridine-5'-diphosphate disodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis.

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

5-OMe-UDP (5-methoxyuridine 5'-trihydrogen diphosphate) is a P2Y6 receptor agonist (EC₅₀=0.08 μM). 5-OMe-UDP activates the P2Y6 receptor by binding to it, which triggers signaling pathways within the cell. This activation can lead to an increase in intracellular calcium ion concentration, which in turn regulates cellular function. The methoxy groups of 5-OMe-UDP provide additional activity and selectivity, contributing to the binding of 5-OMe-UDP to the P2Y6 receptor. 5-OMe-UDP can be used to study diseases related to P2Y6 receptor function, such as diabetes, inflammatory bowel disease, Alzheimer's disease, etc.

Uridine-5'-O-(3-thiotriphosphate) (UTPγS), 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) stimulates inositol phosphate formation in human 1321N1 astrocytoma cells stably expressing the phospholipase C-coupled human P2U-purinoceptor (EC₅₀ = 240 nM).