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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).
AC 1903 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 303.36 |
公式 | C19H17N3O |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 15.17 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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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关键词: AC 1903, AC 1903 supplier, AC1903, selective, TRPC5, blockers, blocks, proteinuria, TRPC, 6766, Tocris Bioscience
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