Fenoldopam mesylate
Based on 4 publication(s) in Google Scholar
Fenoldopam (SKF-82526) mesylate is a selective dopamine D1 receptor agonist. Fenoldopam mesylate binds to rat D1B dopamine receptors (Kd = 11 nM) and human D1A receptors (Kd = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam mesylate modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam mesylate can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 67227-57-0
- Formula: C17H20ClNO6S
- Molecular Weight:401.86
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Fenoldopam mesylate
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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Human D1 Receptor 17 nM (Kd) |
Rat D1 Receptor 11 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| LLC-PK1 | EC50 |
55.5 nM
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2973247 |
Fenoldopam (SKF-82526) (40 min) mesylate competes for specific 125I-Sch 23982 binding sites in rat renal cortical membranes with a Ki of 1,975 nM (Tris-HCl buffer) and 1,895 nM (Dulbecco's buffer)[1].
Fenoldopam (1 nM-6 μM; 72 h) mesylate does not inhibit the proliferation of CD3/CD28-stimulated Jurkat leukemic T cells, in contrast to its inhibitory effect on normal activated T cells[2].
Fenoldopam (1 μM; 5 h) mesylate co-treated Theophylline (HY-B0809) increases intracellular cAMP levels in CD3/CD28-stimulated Jurkat cells[2].
Fenoldopam (1 μM; 10-30 min) mesylate increases DARPP-32 phosphorylation in small cell lung cancer (SCLC) H-69 cells and primary SCLC cultures[3].
Fenoldopam (1 μM; 30 180 min) mesylate induces cAMP accumulation in SCLC cells and increases BrdU incorporation in SCLC H-69 cells as well as primary SCLC cultures (SCLC H-3)[3].
Fenoldopam (0.1 μM; 48 h) mesylate reduces the secretion of TNF-α, IFN-γ, IL-1β, IL-2, IL-4, IL-6, IL-8 and IL-10 by IL-2 activated PBMCs, and downregulates the expression of T cell activation markers CD69, CD28 and intracellular IL-2 in CD3+ T cells from psoriasis patients[4].
Fenoldopam (0.1 μM; 1 h) mesylate reduces the chemotactic migration of CD3/CD28-activated normal human T cells towards SDF-1/CXCL12 by 27-55%[4].
Fenoldopam (0.1 μM; 15 sec) mesylate induces depolarization of resting and activated normal human T cells[4].
Fenoldopam (10 pM-1 μM; 24 h) increases D1 and D3 receptor protein expression in a concentration- and time-dependent manner in rat aortic smooth muscle A10 cells[6].
Fenoldopam (0.1 μM; 24 h) mesylate increases D1/D3 receptor coimmunoprecipitation in A10 cells[6].
Fenoldopam (100 pM-1 mM) mesylate induces vasorelaxation in rat mesenteric arterial rings preconstricted with KCl (Emax = 83%, pED50 = 5.0)[6].
Fenoldopam mesylate binds to rat D1B dopamine receptors with a Kd of 11 nM and human D1A receptors with a Kd of 17 nM in COS-7 cell membranes expressing the cloned receptors[7].
Fenoldopam (1 nM-100 μM; cumulative) mesylate has minimal effect on mouse ductus arteriosus tone, and does not impair O2-or indomethacin-induced ductus constriction[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat leukemic T cells, normal activated T cells
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Concentration:1, 5, 10, 50, 100, 200, 400, 600, 800 nM; 1, 2, 4, 6 μM
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Incubation Time:72 h
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Result:Did not inhibit proliferation of CD3/CD28-stimulated Jurkat cells at any concentration tested.
Inhibited proliferation of normal activated T cells with maximum inhibition at 1 μM.
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Cell Line:SCLC H-69 cells, SCLC primary cultures
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Concentration:1 μM
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Incubation Time:10, 30 min
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Result:Increased DARPP-32 phosphorylation.
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Cell Line:SCLC H-69 cells, SCLC primary cultures (SCLC-H3)
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Concentration:1 μM
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Incubation Time:30, 90, 180 min
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Result:Induced BrdU incorporation in both cell lines.
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Cell Line:CD3/CD28-activated normal human T cells
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Concentration:100 nM
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Incubation Time:1 h pre-incubation + 4 h migration assay
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Result:Reduced chemotactic migration towards SDF-1/CXCL12 by 27-55%.
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Cell Line:A10 cells (rat aortic smooth muscle cells)
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Concentration:10 pM-1 μM
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Incubation Time:24 h (concentration-response); 2, 4, 8, 16, 24, 30 h (time-course)
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Result:Increased D1 and D3 receptor protein expression in a concentration- and time-dependent manner.
Fenoldopam (1, 3, 10 μg/kg; i.v.; 40 min per dose) mesylate increases effective renal plasma flow (ERPF) in a dose-dependent manner in conscious rats, with no significant change in GFR, resulting in a decreased filtration fraction[5].
Fenoldopam (1 mg/kg; i.p.; once hourly for 4 doses) mesylate does not impair postnatal ductus arteriosus closure in newborn CD-1 mice[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Glycine-induced hyperfiltration study in conscious male SD rats (320-360 g)[5]
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Dosage:1 μg/kg
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Administration:i.v.; during glycine infusion
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Result:Reversed glycine-induced glomerular hyperfiltration and reduced GFR from 1.30 to 1.17 mL/100 g/min.
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Animal Model:Dose-response study in conscious male SD rats (320-360 g)[5]
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Dosage:1, 3, 10 μg/kg
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Administration:i.v.; 40 min per dose
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Result:Increased effective renal plasma flow (ERPF) in a dose-dependent manner in conscious rats, with no significant change in GFR, resulting in a decreased filtration fraction.
Chemical Information
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CAS No. 67227-57-0
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Appearance Solid
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Molecular Weight 401.86
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Formula C17H20ClNO6S
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Color White to off-white
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SMILES
OC1=C(O)C=C2C(C3=CC=C(O)C=C3)CNCCC2=C1Cl.CS(=O)(O)=O
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Synonyms
Fenoldopam methanesulfonate; SKF-82526 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell
2021 Feb 18;184(4):943-956.e18. PMID: 33571432 -
SLAS Discov
2020 Sep;25(8):895-905. PMID: 32567455 -
Biochem Biophys Res Commun
2022 Jan 15:588:83-89. PMID: 34953210 -
Biomed Pharmacother
Dopamine receptor agonists ameliorate bleomycin-induced pulmonary fibrosis by repressing fibroblast differentiation and proliferation. [Abstract]2021 Jul:139:111500. PMID: 33901873
Solvent & Solubility
DMSO : ≥ 36 mg/mL (89.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (24.88 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Felder RA, et al. Dopamine1 receptors in rat kidneys identified with 125I-Sch 23982. Am J Physiol. 1988 Nov;255(5 Pt 2):F970-6. [Content Brief]
[2]. Basu B, et al. D1 and D2 dopamine receptor-mediated inhibition of activated normal T cell proliferation is lost in jurkat T leukemic cells. J Biol Chem. 2010 Aug 27;285(35):27026-27032. [Content Brief]
[3]. Cherubini E, et al. Genetic and Functional Analysis of Polymorphisms in the Human Dopamine Receptor and Transporter Genes in Small Cell Lung Cancer. J Cell Physiol. 2016 Feb;231(2):345-56. [Content Brief]
[4]. Keren A, et al. Instantaneous depolarization of T cells via dopamine receptors, and inhibition of activated T cells of Psoriasis patients and inflamed human skin, by D1-like receptor agonist: Fenoldopam. Immunology. 2019 Nov;158(3):171-193. [Content Brief]
[5]. Gillies MA, et al. Fenoldopam to prevent acute kidney injury after major surgery-a systematic review and meta-analysis. Crit Care. 2015 Dec 25;19:449. [Content Brief]
[6]. Zeng C, et al. Dopamine D1 receptor augmentation of D3 receptor action in rat aortic or mesenteric vascular smooth muscles. Hypertension. 2004 Mar;43(3):673-9. [Content Brief]
[7]. Tiberi M, et al. Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor. Proc Natl Acad Sci U S A. 1991 Sep 1;88(17):7491-5. [Content Brief]
[8]. Crockett SL, et al. Role of dopamine and selective dopamine receptor agonists on mouse ductus arteriosus tone and responsiveness. Pediatr Res. 2020 May;87(6):991-997. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4884 mL | 12.4421 mL | 24.8843 mL | 62.2107 mL |
| 5 mM | 0.4977 mL | 2.4884 mL | 4.9769 mL | 12.4421 mL | |
| 10 mM | 0.2488 mL | 1.2442 mL | 2.4884 mL | 6.2211 mL | |
| 15 mM | 0.1659 mL | 0.8295 mL | 1.6590 mL | 4.1474 mL | |
| 20 mM | 0.1244 mL | 0.6221 mL | 1.2442 mL | 3.1105 mL | |
| DMSO | 25 mM | 0.0995 mL | 0.4977 mL | 0.9954 mL | 2.4884 mL |
| 30 mM | 0.0829 mL | 0.4147 mL | 0.8295 mL | 2.0737 mL | |
| 40 mM | 0.0622 mL | 0.3111 mL | 0.6221 mL | 1.5553 mL | |
| 50 mM | 0.0498 mL | 0.2488 mL | 0.4977 mL | 1.2442 mL | |
| 60 mM | 0.0415 mL | 0.2074 mL | 0.4147 mL | 1.0368 mL | |
| 80 mM | 0.0311 mL | 0.1555 mL | 0.3111 mL | 0.7776 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Fenoldopam mesylate Related Classifications
HY-B0735A Related Classifications
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