Fenoldopam mesylate

SKU: orb1221897

Description

Fenoldopam mesylate is a synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is used as an antihypertensive agent. It was approved by the Food and Drug Administration (FDA) in September 1997. Since fenoldopam is the only intravenous agent that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitant renal insufficiency.(In Vitro):Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in the LLC-PK1 cells.Fenoldopam (0-300 μM; 48 or 72 h) displays significant antiproliferative activity against RCC cell lines.Fenoldopam (5 μM and 10 μM; 72 h) induces cell apoptosis in a dose-dependent manner.(In Vivo):Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI).

Key Properties

• CAS Number: 67227-57-0
• MW: 401.86
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₆ClNO₃·CH₄O₃S
• SMILES: CS(O)(=O)=O.OC1=CC=C(C=C1)C1CNCCC2=C(Cl)C(O)=C(O)C=C12
• Target: dopamine-1 receptor
• Solubility: DMSO : ≥ 36 mg/mL 89.58 mM; H2O : 10 mg/mL24.88 mM

Bioactivity

• In Vivo:
  Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can induce arteritis in rats detected by magnetic resonance imaging (MRI). Animal model: Female Sprague-Dawley rats. 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.
• In Vitro:
  Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in the LLC-PK1 cells. Fenoldopam (0-300 μM; 48 or 72 h) displays significant antiproliferative activity against RCC cell lines. Fenoldopam (5 μM and 10 μM; 72 h) induces cell apoptosis in a dose-dependent manner. Cell Proliferation Assay 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Fenoldopam, Corlopam, SK and F-82526J

Quick Database Links

Gene Symbol

dopamine-1 receptor