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Submit ReviewAC 1903 is a selective TRPC5 blocker (IC50 = 4.0 - 13.6 μM). Also displays weak inhibition at TRPC4 (IC50 >100 μM) but not TRPC6. Exhibits no effect against a standard panel of profiling kinases. Blocks TRPC5 channel activity in glomeruli of proteinuric rats. Suppresses severe proteinuria and prevents podocyte loss in a transgenic rat model of focal segmental glomerulosclerosis (FSGS).
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M. Wt | 303.36 |
Formula | C19H17N3O |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 831234-13-0 |
PubChem ID | 667146 |
InChI Key | OECUWHDVQIITIS-UHFFFAOYSA-N |
Smiles | C1(NCC2=CC=CO2)=NC3=CC=CC=C3N1CC4=CC=CC=C4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 15.17 | 50 |
The following data is based on the product molecular weight 303.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 6.59 mL | 32.96 mL | 65.93 mL |
2.5 mM | 1.32 mL | 6.59 mL | 13.19 mL |
5 mM | 0.66 mL | 3.3 mL | 6.59 mL |
25 mM | 0.13 mL | 0.66 mL | 1.32 mL |
References are publications that support the biological activity of the product.
Chung et al (2017) TRP'ing up chronic kidney disease. Science 358 1256 PMID: 29217557
Zhou et al (2017) A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science 358 1332 PMID: 29217578
Minard et al (2018) Remarkable progress with small-molecule modulation of TRPC1/4/5 channels: implications for understanding the channels in health and disease. Cells 7 doi: 10.3390 PMID: 29865154
Sharma et al (2019) Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903. Bioorg.Med.Chem.Lett. 29 155 PMID: 30538066
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Keywords: AC 1903, AC 1903 supplier, AC1903, selective, TRPC5, blockers, blocks, proteinuria, TRPC, 6766, Tocris Bioscience
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