P2Y6 Receptor Antagonist

MRS 2578 is a selective and potent P2Y6 receptor antagonist with IC₅₀s of 37 nM (human) and 98 nM (rat). MRS 2578 exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors.

P2Y6R antagonist 1 (compound 5ab) is a selective, orally active P2Y6R antagonist with an IC₅₀ value of 19.6 nM. P2Y6R antagonist 1 has anti-inflammatory activity.

P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC₅₀ of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis.

MRS4917 is an orally active, potent selective P2Y₁₄ receptor (hP2Y₁₄R) antagonist (IC₅₀ = 2.88 nM, K_i = 1.67 nM) that shows >18,000 fold selectivity against P2Y₆R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.

P2Y1/P2Y6 antagonist 1 (Compound 3h) is an indolesulfonylhydrazide derivative. P2Y1/P2Y6 antagonist 1 is an orally active tP2Y1 and rP2Y6 antagonist (IC₅₀ of 9.72 and 1.89 μM, respectively). P2Y1/P2Y6 antagonist 1 can be used in the study of neurological diseases, inflammation, cardiovascular diseases and cancer.