P2Y14 Receptor Inhibitor

Chloramphenicol succinate sodium is a prodrug of Chloramphenicol (HY-B0239), acting as a P2Y14R inhibitor with an IC₅₀ of 1.585 nM. Chloramphenicol succinate sodium serves as a competitive substrate and inhibitor of succinate dehydrogenase (SDH), which may account for its toxicity. Chloramphenicol succinate sodium exerts a significant inhibitory effect on colitis. Chloramphenicol succinate sodium can be used in research related to myelosuppression, gray baby syndrome, aplastic anemia, bacterial meningitis and inflammatory bowel disease.

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC₅₀ values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y₁₄R (IC₅₀ = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

MRS4654 is an efficient and neutral P2Y14R (hP2Y14R IC₅₀ = 15.0 nM, mP2Y14R IC₅₀ = 18.6 nM) antagonist. MRS4654 has analgesic and anti-inflammatory effects. MRS4654 can be used for research on asthma and neuropathic pain.

MRS4738 is a human P2Y14-targeted inhibitor with an IC₅₀ of 3.11 nM. MRS4738 suppresses inflammatory responses of pulmonary neutrophils and lymphocytes, reduces airway eosinophil accumulation, and alleviates mechanical hyperalgesia. MRS4738 can be applied to the research on the mechanisms of diseases associated with pulmonary inflammation, neuropathic pain and asthma.