产品描述:
TC LPA5 4 is an antagonist of lysophosphatidic acid receptor 5 (LPA5; IC50 = 0.8 µM in McA-RH7777 cells expressing the human receptor).{69589} It selectively inhibits the aggregation of washed isolated human platelets induced by 16:0 alkyl-LPA (1-palmitoyl LPA; Item Nos. 10010094 | 10010290) over collagen or thrombin receptor activating peptide (TRAP; IC50s = 0.8, >10, and >10 µM, respectively). TC LPA5 4 also inhibits the histone-lysine N-methyltransferase NSD2 (IC50 = 8.5 µM) and 29 other methyltransferases (IC50s = 0.33-71 µM).{69590} It reduces tumor volume in a CGTH-W-3 thyroid cancer mouse xenograft model when administered at a dose of 10 mg/kg.{69591} TC LPA5 4 (10 mg/kg, i.p.) prevents brain tissue loss and neurological deficits, as well as increases survival, neurogenesis in the subventricular zone, and angiogenesis in the penumbra, in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO).{69592}