| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Fenoldopam mesyalte (SKF-82526) is a synthetic benzazepine analog acting as a selective D1 receptor partial agonist. The Food and Drug Administration (FDA) authorized it in September 1997 as an antihypertensive medication. Fenoldopam may be helpful in hypertensive patients with concurrent renal insufficiency since it is the only intravenous medication that enhances renal perfusion.
| Targets |
LSD1 ( IC50 = 0.8974 μM )
|
|---|---|
| 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]. |
| 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].
|
| 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). |
| Animal Protocol |
Female Sprague-Dawley rats
100 mg/kg Subcutaneous injection; 100 mg/kg; once daily; 2 days |
| References |
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| Additional Infomation |
Fenoldopam mesylate is a benzazepine.
Fenoldopam Mesylate is the mesylate salt form of fenoldopam, a benzazepine derivative with rapid-acting vasodilator activity. Fenoldopam mesylate is a racemic mixture of S- and R- isomers; the latter is responsible for the biological activity and has a significantly higher affinity for dopamine D1-like receptors (D1 and D5) as well as moderate affinity to alpha-2 adrenergic receptors. This agent selectively activates the dopamine D1-like receptor, thereby causing vasodilatation and increasing renal perfusion. A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. See also: Fenoldopam (has active moiety). |
| Molecular Formula |
C16H16CLNO3
|
|---|---|
| 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
|
| Density |
1.38g/cm3
|
| Boiling Point |
522.6ºC at 760 mmHg
|
| Flash Point |
269.9ºC
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| LogP |
3.776
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
1
|
| 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]
|
| 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)
|
| 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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