p2y14

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-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) is a natural product and a P2Y14 receptor agonist (EC50 = 0.35 μM) with endogenous activity and selectivity. It is used for studying mechanisms related to cardiac inflammation following myocardial infarction/reperfusion injury.

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 5 (Compound A) is a novel P2Y14R antagonist with a benzisoxazole-based structure, exhibiting an IC50 of 23.60 nM and a KD of 7.26 μM. This compound can reduce levels of pro-inflammatory factors (IL-1β, IL-6, TNF-α) and myeloperoxidase (MPO). It demonstrates anti-inflammatory activity in a mouse model of LPS-induced acute lung injury.

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.

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.

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.

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.

HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC50 of 26 pM. HDB-1 shows no significant inhibition on P2Y1R, P2Y2R, P2Y4R, P2Y6R, and P2Y12R. HDB-1 blocks the activation of hepatic stellate cells (HSC) by inhibiting the PKA/Raf1/MEK/ERK signaling pathway mediated by P2Y14R, thereby alleviating the core pathological process of liver fibrosis. HDB-1 is used in liver fibrosis research models to investigate purinergic receptor signaling specificity, hepatic stellate cell activation pathways, and downstream MAPK pathway modulation in fibrogenesis-related cellular systems.

MRS4917 is a potent and selective orally active P2Y14 receptor (hP2Y14R) antagonist, with an IC50 of 2.88 nM and a Ki of 1.67 nM, demonstrating over 18,000-fold selectivity against P2Y6R (IC50= 54 μM). It effectively reverses established mechanical allodynia in a chronic sciatic nerve compression (CCI) mouse model without affecting thermoregulation when administered orally. MRS4917 is applicable for research in neurological disorders.

HDL-16 is a highly effective P2Y14R antagonist with anti-colitis effects, targeting P2Y14R in intestinal epithelial cells to alleviate ulcerative colitis.

UDP-a-D-Galactose disodium salt is a donor substrate for galactosyltransferases employed in the biosynthesis of galactose-containing oligosaccharides[1].

UDP trisodium (Compound 3) is a nucleotide and a P2Y14 receptor agonist, exhibiting an EC50 of 160 nM for the human P2Y14 receptor. It demonstrates greater efficacy compared to the P2Y6 receptor and is utilized in researching pain, diabetes, cystic fibrosis, and other pulmonary disorders.

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.

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.

MRS2690 disodium is a selective agonist of the P2Y14 receptor. It inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and causing concentration-dependent vasoconstriction in porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38, and stimulates [35S]GTPγS binding on the membrane of RBL-2H3 cells. It also enhances the β-hexosaminidase (β-Hex) release induced by antigen (NP-BSA) and C3a. This compound is useful for research in ischemic heart disease.