产品
编 号：F472069
分子式：C19H17N3O
分子量：303.36
分子式：C19H17N3O
分子量：303.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 831234-13-0
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
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