产品描述:
GSK205 is an inhibitor of transient receptor potential vanilloid 4 (TRPV4) and transient receptor potential ankyrin 1 (TRPA1; IC50s = 4.19 and 5.56 µM, respectively, for the rat channels).{68778} It inhibits calcium influx induced by the TRPV4 agonist GSK101 (GSK1016790A; Item No. 17289) in whole-cell patch-clamp assays using Neuro2a neuroblastoma cells expressing TRPV4 when used at a concentration of 5 µM. GSK205 (10 µM) prevents compression-induced increases in NF-κB transcriptional activity and secreted levels of IL-6 and VEGFA, as well as inhibits compression-induced fractures, abnormal cell morphology, and fissures in the intervertebral space, in primary mouse lumbar spines when used at a concentration of 10 µM.{68779}