• 产品描述： AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model

• 靶点： IC50: 14.7 μM (TRPC5 current IN HEK-293 cells);TRP/TRPVChannel

• 体外研究：
  TRPC5 is a Ca2+ permeable nonselective cation channel highly expressed in brain and kidney. AC1903 (0-100 µM) blocks riluzole-activated TRPC5 whole-cell current, but fails to block carbachol (CCh)–induced TRPC4 and OAG-induced TRPC6 currents, even at high micromolar concentrations in Patch-clamp electrophysiology experiments. The ICIC50 values of ML204 (HY-12949) (IC50=13.6 μM) and AC1903 (IC50=14.7 μM) are nearly equipotent in human embryonic kidney 293 (HEK-293) cells expressing TRPC5. AC1903 (30 µM) inhibits angiotensin II-induced production of reactive oxygen species (ROS) in wild-type podocytes and podocytes expressing a mutant angiotensin II type 1 (AT1) receptor that cannot be inactivated and endocytosed. AC1903 (30 µM) blocks caAT1R-induced ROS generation. Increased podocyte cell death within 36 hours of caAT1R expression is observed, but AC1903 protects podocyte cells from cell death. Cell Viability Assay Cell Line: Podocyte cells Concentration: 30 µM Incubation Time: 36 hours Result: Rescued podocyte cell death.

• 体内研究：
  AC1903 (intraperitoneal injection; 50 mg/kg; twice per day; 7 days) significantly suppresses proteinuria as well as reduces pseudocyst formation and podocyte loss in an AT1 receptor transgenic rat model of kidney disease. AC1903 (intraperitoneal injection; 50 mg/kg; twice per day; initiated on day 7 and treated for 1 week until day 14) initiatation on day 7 exhibits significant suppression of proteinuria with preserved podocyte numbers. Besides, AC1903 does not affect the mean arterial pressure (MAP) and exhibits no effect on body weight, blood urea nitrogen, or creatinine in Dahl S rats. Animal Model: Hypertension-induced focal segmental glomerulosclerosis (FSGS) model in Dahl salt-sensitive rats Dosage: 50 mg/kg Administration: Intraperitoneal injection; 50 mg/kg; twice per day; 7 days Result: Inhibited the progression of proteinuric kidney disease by preserving podocytes. Animal Model: 6-week-old Dahl S rats received 2% NaCl for 1 week with severe, progressive proteinuric disease Dosage: 50 mg/kg Administration: Intraperitoneal injection; 50 mg/kg; twice per day; initiated on day 7 and treated for 1 week until day 14 Result: Decreased the rate of proteinuria when administered at the beginning of a high-salt diet and prevents progression when administered one week following initiation of a high-salt diet.

• 参考文献：
  1. Yiming Zhou, et al. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science. 2017 Dec 8;358(6368):1332-1336.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.296 ml	16.482 ml	32.964 ml
  5 mM	0.659 ml	3.296 ml	6.593 ml
  10 mM	0.33 ml	1.648 ml	3.296 ml
  50 mM	0.066 ml	0.33 ml	0.659 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *