AS2717638 is a highly potent, selective, orally active, and brain-penetrant lysophosphatidic acid (LPA) receptor 5 antagonist (IC50 value of 0.038 μM). AS2717638 blunted LPA-induced phosphorylation of STAT1 and STAT3, p65, and c-Jun and consequently reduced the secretion of pro-inflammatory cyto-/chemokines (IL-6, TNFα, IL-1β, CXCL10, CXCL2, and CCL5) at non-toxic concentrations. Moreover, AS271763 modulated the expression of intracellular (COX-2 and Arg1) and plasma membrane-located (CD40, CD86, and CD206) polarization markers and attenuated the neurotoxic potential of LPA-activated BV-2 cell-conditioned medium towards CATH.a neurons.
KEYWORDS: AS2717638 | LPA receptor 5 antagonist | AS 2717638 | AS-2717638 | CAS [2148339-28-8] | LPA | Antagonist | Receptors | Analgesia | Neuropathic and inflammatory pain | Allodynia