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. |
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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. |
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| 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 | 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。 |
