AC1903 - CAS:831234-13-0

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AC1903

目录号 : KM2858 CAS No. : 831234-13-0 纯度 : 98%

Data Sheet 产品使用指南

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。

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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.

体外研究

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 (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.

分子式

C₁₉H₁₇N₃O

分子量

303.36

CAS号

831234-13-0

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (329.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2964 mL	16.4821 mL	32.9641 mL
5 mM	0.6593 mL	3.2964 mL	6.5928 mL
10 mM	0.3296 mL	1.6482 mL	3.2964 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.24 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。