gpr17

P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual antagonist with an IC50 of 3.17 μM for P2Y2R and 1.67 μM for GPR17.

GPR17 antagonist 1 (compound 978) is a GPR17 antagonist utilized for research in diabetes and obesity.

GPR17 Modulator-1 (Compound 2-046) is a regulator of the G protein-coupled receptor 17 (GPR17), displaying an IC50 of less than 10 nM against hGPR17 in CHO cells. This compound exhibits moderate pharmacokinetic properties in mice and possesses the ability to permeate the blood-brain barrier (BBB).

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.

PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.

GPR17 agonist

ASN04421891, a potent GPR17 receptor modulator with an EC50 of 3.67 nM in the [35S]GTPγS binding assay, shows promise for neurodegenerative diseases research[1].

ASN06917370 (Compound V) is a specific modulator of the orphan receptor GPR17 (Uracil Nucleotide/Cysteinyl Leukotriene Receptor), with an EC50 of 268 pM for [35S]GTPyS binding, and exhibits neuroprotective effects.

ASN04885796 (compound IV) is a neuroprotective, specific GPR17 agonist with an EC50=2.27 nM for GPR17-mediated GTPγS binding and can be used to study neurodegenerative diseases such as cerebral ischemia and demyelinating diseases.

UDP-α-D-Glucose sodium hydrate is an endogenous metabolite and a pyrimidine nucleotide sugar, involved in glycosylation reactions during metabolic processes, serving as a precursor and substrate for enzymes in the synthesis of glycogen and sucrose.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

T0510-3657 is a selective activator of GPR17, inhibiting cAMP levels, with potential for playing a key role in the development of a treatment against diseases such as, multiple sclerosis, Parkinson disease, Alzheimer's disease, and cancer.

PSB-1737 is a Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17 (EC50 270 nM).

ASN02563583, a regulator of the GPR17 receptor, exhibits an IC50 value of 0.64 nM in the [35S]GTPγS binding assay and can be utilized in neurological disease research [1].