AC1903|831234-13-0|-陌孚医药/Medlife

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AC1903

目录号: PL12451 纯度: ≥99%

CAS No. :831234-13-0

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中文名称	AC1903
中文别名	1-苄基-N-(呋喃-2-基甲基)-1H-苯并[d]咪唑-2-胺
英文名称	AC1903
英文别名	N-(2-Furanylmethyl)-1-(phenylmethyl)-1H-benzimidazol-2-amine;1-benzyl-N-(furan-2-ylmethyl)-1H-benzimidazol-2-amine;1-benzyl-N-(furan-2-ylmethyl)benzimidazol-2-amine;MLS000084083;1-benzyl-N-[(furan-2-yl)methyl]-1H-1,3-benzodiazol-2-amine;1-benzyl-N-(2-furylmethyl)-1H-benzimidazol-2-amine;SMR000048469;cid_667146;BDBM49021;GTPL10290;HMS1619G06;HMS2402F06;STK227878;VU0217898-5;(1-benzylbenzimidazol-2-yl)-(2-furfuryl)amin;1-Benzyl-N-(furan-2-ylmethyl)-1H-benzo[d]imidazol-2-amine;AC1903
Cas No.	831234-13-0
分子式	C₁₉H₁₇N₃O
分子量	303.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	AC1903 是 TRPC5 的特异性选择性抑制剂，具有足细胞保护特性。AC1903 对 TRPC4 或 TRPC6 current 没有影响，并且在激酶谱分析中没有显示出脱靶效应。在局灶节段性肾小球硬化 (FSGS) 大鼠模型中，AC1903 抑制严重蛋白尿，并且防止足细胞丢失。
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.
性状	Solid
IC50 & Target[1][2]	IC50: 14.7 μM (TRPC5 current IN HEK-293 cells)
体外研究(In Vitro)	TRPC5 is a Ca 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
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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

溶解度数据	In Vitro: DMSO : 100 mg/mL (329.64 mM; Need ultrasonic)配制储备液

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