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).
Specific inhibitor of TRPC5
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | C12=CC=CC=C1N=C(NCC3=CC=CO3)N2CC4=CC=CC=C4 |
| InChI | 1S/C19H17N3O/c1-2-7-15(8-3-1)14-22-18-11-5-4-10-17(18)21-19(22)20-13-16-9-6-12-23-16/h1-12H,13-14H2,(H,20,21) |
| InChI key | OECUWHDVQIITIS-UHFFFAOYSA-N |
