Non disponible en dehors du Royaume-Uni et de l'Irlande
Application
AC1903 has been used as a drug candidate in a high-throughput agar colony formation assay to identify its therapeutic efficiency against medulloblastoma.
Biochem/physiol Actions
AC1903 is a specific inhibitor of TRPC5, the transient receptor potential canonical channel 5, a Ca2+ permeable nonselective cation channel highly expressed in brain and kidney. AC1903 did not inhibit TRPC4 or TRPC6 currents and showed no off-target effects in kinase profiling assays. It specifically blocked TRPC5 channel activity in glomeruli of proteinuric rats, suppressed severe proteinuria, showing a therapeutic benefit in a rat model of hypertensive proteinuric kidney disease.
Chronic administration of AC1903 averts the loss of podocytes in a transgenic rat model of focal segmental glomerulosclerosis (FSGS).
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