Fenoldopam mesylate

立即咨询

Fenoldopam mesylate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

67227-57-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

非诺多泮甲磺酸盐
Fenoldopam methanesulfonate
SKF-82526 mesylate

产品介绍

Fenoldopam mesylate (SKF-82526) 是一种D₁receptor激动剂和新型的lysine-specific demethylase 1(LSD1) 抑制剂 (IC₅₀=0.8974 μM)。Fenoldopam mesylate 具有抗高血压和抗癌细胞增殖的活性，并能诱导细胞凋亡。

生物活性

Fenoldopam mesylate (SKF-82526) is aD₁receptoragonist and a novellysine-specific demethylase 1(LSD1) inhibitor (IC₅₀=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cellsapoptosis^[1]^[2]^[3].

IC₅₀& Target

IC50: 0.8974 μM (LSD1)^[2]

体外研究
(In Vitro)

Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in the LLC-PK1 cells^[1].
Fenoldopam (0-300 μM; 48 or 72 h) displays significant antiproliferative activity against RCC cell lines^[2].
Fenoldopam (5 μM and 10 μM; 72 h) induces cell apoptosis in a dose-dependent manner^[2].

Cell Proliferation Assay^[1]

Cell Line:	786-O, ACHN, and HK-2 cells
Concentration:	0-300 μM
Incubation Time:	48 or 72 hours
Result:	Inhibited the growth of ACHN cells (IC₅₀=16.55 μM, 48 h; IC₅₀=10.34 μM, 72 h), 786-O cells (IC₅₀=57.89 μM, 48 h; IC₅₀=47.52 μM, 72 h), and HK2 cells (IC₅₀>300 μM, 48h and 72 h).

Apoptosis Analysis^[1]

Cell Line:	ACHN cells
Concentration:	5 μM and 10 μM
Incubation Time:	72 hours
Result:	Increased apoptotic cells from at 2.2% (control) to 47.7% (5 μM, fenoldopam) and 60.8% (10 μM, fenoldopam), respectively.

体内研究
(In Vivo)

Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI)^[3].

Animal Model:	Female Sprague-Dawley rats^[3]
Dosage:	100 mg/kg
Administration:	Subcutaneous injection; 100 mg/kg; once daily; 2 days
Result:	Showed low-intensity areas and a high signal intensity region around the artery, and these findings were considered to be erythrocytes infiltrating the arterial wall and perivascular edema, respectively. Observed perivascular edema histopathologically.

Clinical Trial

分子量

401.86

性状

Solid

Formula

C₁₇H₂₀ClNO₆S

CAS 号

67227-57-0

中文名称

非诺多泮甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 36 mg/mL(89.58 mM)

H₂O : 10 mg/mL(24.88 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4884 mL	12.4421 mL	24.8843 mL
5 mM	0.4977 mL	2.4884 mL	4.9769 mL
10 mM	0.2488 mL	1.2442 mL	2.4884 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。