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经验公式(希尔记法):
C19H17N3O
化学文摘社编号:
分子量:
303.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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
SMILES string
C12=CC=CC=C1N=C(NCC3=CC=CO3)N2CC4=CC=CC=C4
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Yiming Zhou et al.
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.
Mohammed Sedeeq et al.
Pharmaceuticals (Basel, Switzerland), 13(11) (2020-11-11)
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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