P2Y Receptor Agonist

NF546 (hydrate) is a selective non-nucleotide P2Y11 agonist with a pEC₅₀ of 6.27. NF546 (hydrate) stimulates release of interleukin-8 from human monocyte-derived dendritic cells.

Uridine 5'-diphosphate-¹³C₉,¹⁵N₂ (UDP-¹³C₉,¹⁵N₂) dilithium is the ¹³C₉,¹⁵N₂-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 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y₂ receptor agonist with an EC₅₀ of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y₄ (EC₅₀ of 9.3 μM) and P2Y₆ (EC₅₀ of 7.0 μM) receptors.

2-Thio-UTP tetrasodium is a potent P2Y₂, P2Y₄ and P2Y₆ agonist, which an be used for the research of cancer.

NF546 is a selective non-nucleotide P2Y11 agonist with a pEC₅₀ of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells.

Uridine 5'-diphosphate-d₁₂ (UDP-d₁₂) dilithium is the d₁₂-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.

Uridine-5'-O-(3-thiotriphosphate) trisodium, a stable analogue of UTP, is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability.

ATP-γ-S (tetrasodium) is a P2Y11 receptor agonist, an antioxidant and a neuroprotective agent. ATP-γ-S (tetrasodium) can be used as a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A. ATP-γ-S (tetrasodium) is active in ATP hydrolysis.

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.

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.

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.

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.

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.

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).

MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 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. MRS2690can be used for ischemic heart disease.

MRS2693 trisodium is a selective P2Y6 agonist with an EC₅₀ value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model.

2-MeS-ATP (2-Methylthio-ATP) is an analog of adenosine nucleotides and acts as a P2Y purinergic receptor agonist specific for adenosine nucleotide activation. 2-MeS-ATP is also able to inhibit the release of toxic mediators from macrophages stimulated by endotoxin (LPS). 2-MeS-ATP can be used in the study of endotoxin shock and inflammatory diseases.