p2y14

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-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.

Uridine 5′-diphosphoglucose disodium salt (UDP-Glucose sodium salt) is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It is an agonist of the P2Y14 receptor (EC50 = 0.35 μM) and can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.

P2Y14 antagonist 1 (compound 45) is a highly selective and orally active P2Y14 receptor antagonist with an IC50 value of 0.70 nM. It demonstrates significant anti-inflammatory effects by effectively reducing pulmonary infiltration of immune cells and inflammatory responses through the inhibition of the NLRP3 signaling pathway. P2Y14 antagonist 1 is suitable for studying acute lung injury.

P2Y14R antagonist 3 (compound A) is an orally active P2Y14R antagonist with an IC50 of 23.60 nM and a Kd of 7.26 μM. It mitigates lung injury in mice induced by Lipopolysaccharides (LPS) and can be utilized in the study of inflammatory diseases.

Compound 25l, also known as P2Y14R antagonist 4, is an orally active antagonist of the P2Y14R receptor with an IC50 of 5.6 nM. It exhibits higher binding affinity for P2Y14R compared to other PPTN receptors. P2Y14R antagonist 4 also possesses anti-inflammatory properties, reducing the release of pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α) induced by LPS.

P2Y14R antagonist 2 (compound 39) is an effective and selective orally-active antagonist of P2Y14R with an IC50 of 0.40 nM. It exhibits anti-inflammatory properties and holds potential for use in studying colitis.

P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis.

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

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 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).

Uridine diphosphate glucose (UDP-glucose) is a pyrimidine nucleotide sugar, serving as a precursor for oligosaccharides, polysaccharides, glycoproteins, and glycolipids containing glucose. It is a key intermediate in carbohydrate metabolism and participates in numerous enzymatic reactions, acting as a P2Y14 agonist.

MRS4865 (compound 7a) serves as a chimeric antagonist for the P2Y14 receptor and an agonist for UDP-glucose, offering protection against neuropathic pain.

MRS4833 (compound 15) is an orally active, potent, competitive antagonist of P2Y14R, exhibiting IC50 values of 5.92 nM for hP2Y14R and 4.8 nM for mP2Y14R. It reduces airway eosinophilia in protease-mediated asthma models and reverses chronic neuropathic pain in mouse CCI models.

MRS4608 is a novel and potent antagonist of the P2Y14 receptor.

MRS4654 is an innovative and potent antagonist of the P2Y14 receptor, featuring an IC50 of 15 nM.

MRS2905 (α,β-Methylene-2-thio-UDP) trisodium is a selective P2Y14R agonist with an EC50 of 0.92 nM. It shows no activity on UDP-activated P2Y6 receptors or other P2Y receptors.

P2Y14 receptor agonist

MRS4458 is an effective inhibitor of the P2Y14 Receptor.

MRS4478 is an effective inhibitor of the P2Y14 Receptor.

PPTN Mesylate is an effective and highly selective antagonist of the P2Y14 receptor.

MRS2802 is a P2Y14 receptor agonist, its EC50 value for P2Y14 receptor is 63 nM.

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

MRS2690 is a potent P2Y14 receptor agonist (EC50 = 49 nM) that displays 7-fold higher potency than UDP-glucose.