AC1903 has been used as a drug candidate in a high-throughput agar colony formation assay to identify its therapeutic efficiency against medulloblastoma.[1]
Biochem./physiol. Wirkung
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).[2]
Science (New York, N.Y.), 358(6368), 1332-1336 (2017-12-09)
Progressive kidney diseases are often associated with scarring of the kidney's filtration unit, a condition called focal segmental glomerulosclerosis (FSGS). This scarring is due to loss of podocytes, cells critical for glomerular filtration, and leads to proteinuria and kidney failure.
Medulloblastoma (MB) is the most common malignant childhood brain cancer. High-risk MB tumours have a high incidence of metastasis and result in poor patient survival. Drug screens, commonly used to identify potential novel therapeutic agents against MB, focus on 2D
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