GSK205 (hydrobromide)

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). It inhibits calcium influx induced by the TRPV4 agonist GSK101 (GSK1016790A, Cay-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-kappaB 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.Formal Name: N-[4-[2-[methyl(phenylmethyl)amino]ethyl]phenyl]-5-(3-pyridinyl)-2-thiazolamine, hydrobromide. Molecular Formula: C24H24N4S . XHBr. Formula Weight: 400.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble: 0.1-1 mg/ml. SMILES: CN(CC1=CC=CC=C1)CCC(C=C2)=CC=C2NC3=NC=C(C4=CN=CC=C4)S3.Br. InChi Code: InChI=1S/C24H24N4S.BrH/c1-28(18-20-6-3-2-4-7-20)15-13-19-9-11-22(12-10-19)27-24-26-17-23(29-24)21-8-5-14-25-16-21./h2-12,14,16-17H,13,15,18H2,1H3,(H,26,27).1H. InChi Key: LQGOJHGNGSOUKL-UHFFFAOYSA-N.