Niclosamide (ethanolamine salt) (Synonyms: BAY-73, BAY-6076, Bayluscide, HL 2448) |
| Katalog-Nr.GC44400 |
Niclosamide (ethanolamine salt) ist ein anthelmintisches Medikament, das von der US-amerikanischen Food and Drug Administration (FDA) zur Behandlung von Darminfektionen mit Bandwürmern zugelassen ist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1420-04-8
Sample solution is provided at 25 µL, 10mM.
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Niclosamide (ethanolamine salt) ist ein anthelmintisches Medikament, das von der US-amerikanischen Food and Drug Administration (FDA) zur Behandlung von Darminfektionen mit Bandwürmern zugelassen ist [1,2]. Der Wirkmechanismus des Medikaments besteht darin, die Mitochondrien der parasitären Würmer zu entkoppeln [1,2], und es hat ein ausgezeichnetes Sicherheitsprofil. Niclosamide (Ethanolaminsalz) ist eine Salzform von Niclosamide, die eine höhere Wasserlöslichkeit aufweist [1-3].
Niclosamide hemmte dosisabhängig die STAT3-abhängige Luciferase-Reporteraktivität mit einem IC50 von 0,25 ± 0,07 µM [4]. Niclosamide hemmt die durch den vollständigen Agonisten (Wnt) induzierte Wnt/Frizzled-Signalübertragung mit einem IC50 von 0,5 ± 0,05 µM [5].
Niclosamide hemmte stark die Proliferation und Koloniebildung von Du145-Prostatakrebszellen mit IC50-Werten von 0,7 und 0,1 µM. Niclosamide induzierte dosisabhängig eine G0/G1-Phasenarretierung und Apoptose der Du145-Krebszellen [4]. Niclosamide hemmte die Zellviabilität von drei adrenokortikalen Karzinomzelllinien (ACC) BD140A, SW-13 und NCI-H295R mit IC50-Werten von 0,12 µM, 0,15 µM und 0,53 µM, jeweils [6].
Niclosamide (Ethanolaminsalz) (1.500 ppm in HFD (High-Fat-Diät)) reduzierte signifikant die Nüchternglukosekonzentrationen bei Mäusen mit HFD für 4 Monate [3]. Niclosamide (Ethanolaminsalz) wird schnell von der Leber metabolisiert, mit einer Halbwertszeit von etwa 1,5 Stunden und keiner Akkumulation im Körper nach mehreren Stunden [3]. Die LD50 von Niclosamide (Ethanolaminsalz) bei Ratten beträgt 10.000 mg kg-1 Körpergewicht [3]. Orales Niclosamide hemmte das Tumorwachstum und die Progression von menschlichem Eierstockkrebs und Darmkrebs in Xenograft-Tiermodellen [7,8].
References:
[1]. Frayha G J, Smyth J D, Gobert J G, et al. The mechanisms of action of antiprotozoal and anthelmintic drugs in man[J]. General Pharmacology: The Vascular System, 1997, 28(2): 273-299.
[2]. Sheth U K. Mechanisms of anthelmintic action[J]. Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrès des recherches pharmaceutiques, 1975: 147-157.
[3]. Tao H, Zhang Y, Zeng X, et al. Niclosamide ethanolamine–induced mild mitochondrial uncoupling improves diabetic symptoms in mice[J]. Nature medicine, 2014, 20(11): 1263-1269.
[4]. Ren X, Duan L, He Q, et al. Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway[J]. ACS medicinal chemistry letters, 2010, 1(9): 454-459..
[5]. Chen M, Wang J, Lu J, et al. The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling[J]. Biochemistry, 2009, 48(43): 10267-10274.
[6]. Satoh K, Zhang L, Zhang Y, et al. Identification of Niclosamide as a Novel Anticancer Agent for Adrenocortical CarcinomaNiclosamide in Adrenal Cancer[J]. Clinical Cancer Research, 2016, 22(14): 3458-3466.
[7]. King M L, Lindberg M E, Stodden G R, et al. WNT7A/β-catenin signaling induces FGF1 and influences sensitivity to niclosamide in ovarian cancer[J]. Oncogene, 2015, 34(26): 3452-3462.
[8]. Osada T, Chen M, Yang X Y, et al. Antihelminth Compound Niclosamide Downregulates Wnt Signaling and Elicits Antitumor Responses in Tumors with Activating APC MutationsNiclosamide Inhibits Wnt Signaling and Colorectal Cancer Growth[J]. Cancer research, 2011, 71(12): 4172-4182.
| Cell experiment [1]: | |
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Cell lines |
HeLa cells |
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Preparation Method |
Cells were plated in 96-well culture plates with cell density of 3000-4000 cells/well and treated with indicated compounds by adding 100µL medium containing Niclosamide (ethanolamine salt) of various concentrations on the second day. After 72-hour's treatment, MTT was added to each well and incubated for additional 4-5 hours, and the absorbance was measured on a microplate reader at 570nm. Cell growth inhibition was evaluated as the ratio of the absorbance of the sample to that of the control. |
|
Reaction Conditions |
0.5-5µM for 72 hours |
|
Applications |
Niclosamide dose dependently inhibited STAT3-dependent luciferase reporter activity with an IC50 of 0.25 ± 0.07 µM. |
| Animal experiment [2]: | |
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Animal models |
NOD/SCID mice |
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Preparation Method |
HCT116 cells were harvested from flasks with 0.05% trypsin/EDTA and resuspended with Hank's buffered solution (5 × 106 cells/100 µL). CRC explants (CRC039) cultured in vitro were harvested with the same procedure and mixed with equal volume of Matrigel to make 1 × 106 cells/100 µL concentration. The cell suspensions (100 µL) were inoculated into the flanks of NOD/SCID mice. Four days later, niclosamide administration by gavage 6 d/wk for 2 (HCT116) or 3 weeks (CRC039) began. Tumor size was measured 3 times a week until mice were euthanized. |
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Dosage form |
Niclosamide (10, 100, and 200 mg/kg) was administered by gavage for 6 d/wk for 2 (HCT116) or 3 weeks (CRC039). |
|
Applications |
In the more rapidly growing tumor (HCT116), a dose of 200 mg/kg of body weight was needed to suppress the tumor growth; 100 mg/kg of niclosamide could suppress the growth of the relatively slow-growing tumor (CRC039) to the same level. |
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References: [1]: Ren X, Duan L, He Q, et al. Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway[J]. ACS medicinal chemistry letters, 2010, 1(9): 454-459. |
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| Cas No. | 1420-04-8 | SDF | |
| Überlieferungen | BAY-73, BAY-6076, Bayluscide, HL 2448 | ||
| Canonical SMILES | OC1=C(C(NC2=CC=C([N+]([O-])=O)C=C2Cl)=O)C=C(Cl)C=C1.NCCO | ||
| Formula | C13H8Cl2N2O4•C2H7NO | M.Wt | 388.2 |
| Löslichkeit | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL,Ethanol: 0.25 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.576 mL | 12.88 mL | 25.7599 mL |
| 5 mM | 0.5152 mL | 2.576 mL | 5.152 mL |
| 10 mM | 0.2576 mL | 1.288 mL | 2.576 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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