Catalog No.: PC-23606Not For Human Use, Lab Use Only.
AS2717638 a potent, selective lysophosphatidic acid receptor 5 (LPA5, LPAR5) antagonist, inhibits LPA-induced cAMP accumulation in CHO cells expressing human LPA5 with IC50 of 38 nM.
AS2717638 a potent, selective lysophosphatidic acid receptor 5 (LPA5, LPAR5) antagonist, inhibits LPA-induced cAMP accumulation in CHO cells expressing human LPA5 with IC50 of 38 nM. AS2717638 shows no activity against LPA-induced Ca2+ mobilization in cells expressing human LPA1, LPA2, and LPA3. AS2717638 shows binding Ki of for 9.1, 16 and 7.3 nM for human, rat, and mouse LPA5 receptor respectively. Oral administration of AS2717638 inhibited LPA5 agonist-induced allodynia in mice. AS2717638 also significantly improved PGE2-, PGF2α-, and AMPA-induced allodynia, AS2717638 significantly ameliorated static mechanical allodynia and thermal hyperalgesia in rat models of chronic constriction injury (CCI)-induced neuropathic pain. AS2717638 also showed analgesic effects in a rat model of inflammatory pain.
