Fenoldopam mesylate

• CAT Number: A000068
• CAS Number: 67227-57-0
• Molecular Formula: C17H20ClNO6S
• Molecular Weight: 401.86
• Purity: ≥95%
• Synonyms: 9-chloro-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;methanesulfonic acid
• InChI: InChI=1S/C16H16ClNO3.CH4O3S/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21;1-5(2,3)4/h1-4,7,13,18-21H,5-6,8H2;1H3,(H,2,3,4)
• InChIKey: CVKUMNRCIJMVAR-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)O.C1CNCC(C2=CC(=C(C(=C21)Cl)O)O)C3=CC=C(C=C3)O

Fenoldopam mesylate (SKF-82526) is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis[1][2][3].
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].
Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI)[3].

Reference

[1]. A Grenader, et al. Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells. J Pharmacol Exp Ther. 1991 Jul 1;258(1):193-8.
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[2]. Yan Zheng, et al. Identification of fenoldopam as a novel LSD1 inhibitor to abrogate the proliferation of renal cell carcinoma using drug repurposing strategy. Bioorg Chem. 2021 Mar;108:104561.
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[3]. Yuta Fujii, et al. Detection of fenoldopam-induced arteritis in rats using ex vivo / in vivo MRI. Toxicology Reports, Volume 9, 2022, Pages 1595-1602.