Niclosamide (ethanolamine salt) (Synonyms: BAY-73, BAY-6076, Bayluscide, HL 2448) |
Catalog No.GC44400 |
Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research.
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.
Niclosamide is an anthelmintic drug approved by the US Food and Drug Administration (FDA) for treating intestinal infections of tapeworms [1,2]. The mechanism of action of the drug is to uncouple the mitochondria of the parasitic worms [1,2], and it has an excellent safety profile. Niclosamide (ethanolamine salt) is a salt form of niclosamide that has higher water solubility [1-3].
Niclosamide dose dependently inhibited STAT3-dependent luciferase reporter activity with an IC50 of 0.25 ± 0.07 µM [4]. Niclosamide inhibits Wnt/Frizzled signalling induced by the complete agonist (Wnt) with IC50 of 0.5 ± 0.05 µM [5].
Niclosamide strongly inhibited the proliferation and colony formation of Du145 prostate cancer cells with IC50 values of 0.7 and 0.1 µM. Niclosamide dose dependently induced G0/G1 phase arrest and apoptosis of Du145 cancer cells [4]. Niclosamide inhibited cell viability of 3 Adrenocortical carcinoma (ACC) cell lines BD140A, SW-13, and NCI-H295R with IC50s of 0.12 µM, 0.15 µM, and 0.53 µM, respectively [6].
Niclosamide (ethanolamine salt) (1,500 ppm in HFD(high-fat diet)) significantly reduced fasting blood glucose concentrations in mice with HFD for 4 months [3]. Niclosamide (ethanolamine salt) is rapidly metabolized by the liver, with a half-life of about 1.5 h and no accumulation in the body after several hours [3].The LD50 of Niclosamide (ethanolamine salt) in rats is 10,000 mg kg-1 body weight [3].Oral niclosamide inhibited tumor growth and the progression of human ovarian cancer and colon cancer in xenograft animal models [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.
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