p2y6 receptor

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 (Uridin) is a nucleoside compound, one of the four bases that make up RNA, that replaces thymine in DNA during transcription and pairs with adenine.

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

Uridine 5'-diphosphate sodium salt is a selective native agonist of the P2Y6 receptor (EC50: 300 nM; pEC50: 6.52) and a potent antagonist of P2Y14 (pEC50: 7.28).

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) .

P2Y6R antagonist 1 (compound 5ab) is a selective, orally active antagonist of P2Y6R, featuring an IC50 value of 19.6 nM. This compound also exhibits anti-inflammatory properties.

Potent P2Y6 agonist

MRS 2693 trisodium salt is a P2Y6 agonist.

P2Y6 receptor agonist

MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a

Potent and selective P2Y14 receptor agonist (EC50 = 0.92 nM). Exhibits >2000-fold selectivity over P2Y6. Das et al (2010) Human P2Y14 receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups J.Med.Chem. 53 471 PMID:19902968 |Lazarowski et al (2015) UDP-sugars as extracellular signaling molecules: cellular and physiologic consequences of P2Y14 receptor activation. Mol.Pharmacol. 88 151 PMID:25829059

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.

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].

Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [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.

Uridine 5'-methylenediphosphate (UMP-CP), a hydrolytically stable derivative of UDP and agonist of the purinergic P2Y14 receptor, exhibits selective inhibition of cAMP production in cells expressing human P2Y14 compared to those expressing human P2Y6, with EC50 values of 11 nM and 339 nM, respectively.

Uridine 5'-O-thiodiphosphate (UDP-β-S) is a stable analog of UDP, serving as a selective agonist for the P2Y6 receptor with enhanced metabolic stability, utilized in cardiovascular disease research.