For research use only. Not for therapeutic Use.
GFB-8438(CAT: I016917) is a potent and selective inhibitor of TRPC5 channels, with IC₅₀ values of 0.18 μM for hTRPC5 and 0.29 μM for hTRPC4, while showing excellent selectivity over TRPC6, other TRP family members, NaV1.5, and minimal activity at the hERG channel. In vitro, GFB-8438 (1 μM) protects mouse podocytes from protamine sulfate–induced injury by preventing synaptopodin loss and cytoskeletal remodeling. In vivo, GFB-8438 (30 mg/kg; s.c.; 3 weeks) significantly reduces proteinuria in a hypertensive DOCA-salt rat model of FSGS. Pharmacokinetic profiling (1 mg/kg; i.v.) reveals clearance of 31 mL/min/kg, Vss of 1.17 L/kg, and half-life of 0.5 h.
| CAS Number | 2304549-73-1 |
| Synonyms | 5-chloro-4-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]-1H-pyridazin-6-one |
| Molecular Formula | C16H14ClF3N4O2 |
| Purity | ≥95% |
| IUPAC Name | 5-chloro-4-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]-1H-pyridazin-6-one |
| InChI | InChI=1S/C16H14ClF3N4O2/c17-14-12(7-21-22-15(14)26)23-5-6-24(13(25)9-23)8-10-3-1-2-4-11(10)16(18,19)20/h1-4,7H,5-6,8-9H2,(H,22,26) |
| InChIKey | MITRKIWBJVJRAM-UHFFFAOYSA-N |
| SMILES | C1CN(C(=O)CN1C2=C(C(=O)NN=C2)Cl)CC3=CC=CC=C3C(F)(F)F |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
