p2yreceptor

PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.

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.

Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [1].

4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4. It is utilized in crosslinking experiments and labeling of transcriptional complexes [1] [2].

YM-254890, a macrocyclohexapeptide isolated from Chromobacterium sp, is a selective and potent inhibitor of Gαq 11 protein, inhibits ADP-induced platelet aggregation and inhibits G protein signaling.

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].

NF546 (hydrate), a selective non-nucleotide P2Y11 agonist, exhibits a pEC50 value of 6.27 and induces interleukin-8 secretion from human monocyte-derived dendritic cells [1].

4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetrasodium functions as a potent agonist at P2Y 2 and P2Y 4 receptors, with half-maximal effective concentrations (EC50s) of 35 nM for hP2Y 2 and 350 nM for hP2Y 4. This compound is applicable in studies involving crosslinking experiments and labeling of the transcriptional complex [1] [2].

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.

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.

PSB-0739 Selective platelet P2Y12 receptor antagonist characterized by competitive binding and high affinity (Ki =24.9 nM) with antithrombotic and platelet aggregation modulating effects.

2-Methylthioadenosine diphosphate trisodium (2-MeS-ADP) is the salt form of 2-Methylthioadenosine diphosphate, a synthetic analog of adenosine diphosphate (ADP), a potent purinergic P2Y receptor agonist that agonizes human P2Y13 at nanomolar levels, mouse P2Y13 and human P2Y12, induces platelet aggregation and morphological changes, and is indicated for neurological and cardiovascular disease studies.

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.

Tuberculosis inhibitor 3 (compound 2i) is a highly potent and orally bioavailable anti-tuberculosis drug with in vitro antidrug activity of MIC < 0.016 μg mL against both drug-sensitive and drug-resistant Mycobacterium tuberculosis, H37RV & MDR-TB.

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.

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.

NSC380324 is a P2Y12 receptor antagonist with antiplatelet properties, which can be employed in research on atherosclerotic cardiovascular diseases.

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

Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.

SYL-4 is a potential P2Y12 receptor antagonist with a Ki value of 7.35 ± 1.72 for use in synthetic dyes.

N6-(4-Hydroxybenzyl)adenosine (Para-topolin riboside) is a platelet aggregation inhibitor.

Regrelor disodium (INS 50589) is a P2Y12 receptor antagonist that prevents thrombosis, effectively inhibits vascular smooth muscle cell contraction, curbs cell proliferation, and reduces inflammation.

Ticagrelor (AR-C 126532XX), produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).