Niclosamide (ethanolamine salt) (Synonyms: BAY-73, BAY-6076, Bayluscide, HL 2448) |
| カタログ番号GC44400 |
ニクロサミド (BAY2353) オラミンは、寄生虫感染の研究に使用される経口活性駆虫剤です。
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 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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