| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
LSD1 ( IC50 = 0.8974 μM )
Fenoldopam targets the dopamine D1 receptor, acting as a partial agonist. It also inhibits lysine-specific demethylase 1 (LSD1) with an IC50 of 0.8974 μM. By activating D1 receptors, it induces vasodilation in peripheral arteries, including the renal, coronary, and cerebral arteries. Its antihypertensive effect is mediated through this vasodilation. |
|---|---|
| ln Vitro |
Fenoldopam is a weak partial agonist that is associated with the production of cAMP in LLC-PK1 cells by DA1 receptors[1].
Fenoldopam (0-300 μM; 48 or 72 h) exhibits strong antiproliferative activity against RCC cell lines[2]. Fenoldopam (5 μM and 10 μM; 72 h) causes cell apoptosis in a dose-dependent manner[2]. In vitro, Fenoldopam is a partial agonist with low efficacy at DA1 receptors linked to cAMP generation in LLC-PK1 cells. It displays significant antiproliferative activity against renal cell carcinoma (RCC) cell lines. At concentrations of 5 and 10 μM, it induces cell apoptosis in a dose-dependent manner. It inhibits the growth of ACHN cells (IC50=10.34 μM, 72 h). |
| ln Vivo |
Fenoldopam mesylate (subcutaneous injection; 100 mg/kg; once daily; 2 d) can cause a rat's arthritis, which can be seen on magnetic resonance imaging (MRI)[3].
In vivo, Fenoldopam mesylate shows antihypertensive effects. It induces vasodilation and improves renal perfusion. The compound also demonstrates anti-cancer cell proliferation activity and can induce apoptosis in vivo. It is used as an intravenous antihypertensive agent for the treatment of severe hypertension. |
| Enzyme Assay |
In vitro enzyme assays for Fenoldopam typically measure its inhibition of LSD1. The enzyme is incubated with a histone substrate in the presence of varying concentrations of the compound. Demethylation activity is measured, and IC50 values are calculated. Radioligand binding assays are used to assess its affinity for the D1 receptor.
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| Cell 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). Cellular assays for Fenoldopam are performed using renal cell carcinoma cell lines (e.g., 786-O, ACHN). Cells are treated with the compound at concentrations ranging from 0-300 μM for 48 or 72 hours. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Apoptosis is analyzed by flow cytometry using Annexin V staining. |
| Animal Protocol |
Female Sprague-Dawley rats
100 mg/kg Subcutaneous injection; 100 mg/kg; once daily; 2 days In vivo animal studies with Fenoldopam are conducted in hypertensive animal models. The compound is administered intravenously, and blood pressure and heart rate are monitored. Its effects on renal blood flow and renal function are assessed. In cancer models, its antitumor activity can be evaluated. |
| ADME/Pharmacokinetics |
Fenoldopam is administered intravenously and has a rapid onset of action. It has a short half-life, requiring continuous infusion for sustained antihypertensive effect. It is metabolized in the liver and excreted in urine. Its pharmacokinetic profile is consistent with its use as an acute, hospital-based antihypertensive agent.
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| Toxicity/Toxicokinetics |
Fenoldopam is generally well tolerated but can cause side effects including headache, flushing, hypotension, and tachycardia. It is contraindicated in patients with known hypersensitivity. It should be used with caution in patients with glaucoma or increased intraocular pressure.
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| References |
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| Additional Infomation |
Fernodopam mesylate is a benzodiazepine drug. Fernodopam mesylate is the mesylate salt form of fenodopam, a benzodiazepine derivative with rapid vasodilatory activity. Fernodopam mesylate is a racemic mixture of S- and R-isomers; the latter is the predominantly active component, exhibiting significantly higher affinity for dopamine D1-like receptors (D1 and D5) and moderate affinity for α2-adrenergic receptors. This drug selectively activates dopamine D1-like receptors, thereby causing vasodilation and increasing renal perfusion. It is a dopamine D1 receptor agonist used as an antihypertensive drug. It lowers blood pressure by dilating small arteries. See also: Fernodopam (with active fraction).
Fenoldopam mesylate is a selective dopamine D1 receptor agonist and an LSD1 inhibitor. It is approved by the FDA as an intravenous antihypertensive agent. The compound is also being investigated for its anti-cancer cell proliferation activity. It is the only intravenous drug that improves renal perfusion. |
| Molecular Formula |
C16H16CLNO3
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|---|---|
| Molecular Weight |
401.860
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| Exact Mass |
401.07
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| Elemental Analysis |
C, 50.81; H, 5.02; Cl, 8.82; N, 3.49; O, 23.89; S, 7.98
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| CAS # |
67227-57-0
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| Related CAS # |
Fenoldopam hydrochloride; 181217-39-0; Fenoldopam; 67227-56-9
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| PubChem CID |
49659
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| Appearance |
White to off-white solid powder
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| Density |
1.38g/cm3
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| Boiling Point |
522.6ºC at 760 mmHg
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| Flash Point |
269.9ºC
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| LogP |
3.776
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
26
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(=C(C([H])=C2C=1C([H])([H])C([H])([H])N([H])C([H])([H])C2([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H])O[H])O[H].S(C([H])([H])[H])(=O)(=O)O[H]
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| InChi Key |
CVKUMNRCIJMVAR-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
9-chloro-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;methanesulfonic acid
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| Synonyms |
SKF 82526J; SKF82526J; SKF-82526J; Fenoldopam mesylate; Corlopam
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~80 mg/mL (~199.1 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00621790 | Completed | Drug: fenoldopam Drug: placebo |
Acute Renal Failure | Università Vita-Salute San Raffaele |
February 2008 | Phase 3 |
| NCT00982527 | Completed | Drug: Placebo Drug: Fenoldopam |
Kidney Failure, Acute | Bambino Gesù Hospital and Research Institute |
September 2009 | Phase 3 |
| NCT00122018 | Completed | Drug: N-acetylcysteine Drug: fenoldopam |
Kidney Failure, Acute Kidney Failure, Chronic |
Linda F. Barr, M.D. | May 2002 | Phase 2 |
| NCT00747331 | Completed | Drug: Fenoldopam mesilate Drug: Placebo |
Cardiac Complications Cardiopulmonary Bypass |
IRCCS Policlinico S. Donato | September 2008 | Phase 4 |
| September 2008 | Completed | Drug: Fenoldopam | Salt-sensitive Hypertension | Georgetown University | November 2002 | Not Applicable |
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