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Pyrvinium pamoate (Pyrvinium embonate) Sale

(Synonyms: 扑蛲灵,Pyrvinium embonate) 目录号 : GC32698

An anthelmintic and anticancer agent

Pyrvinium pamoate (Pyrvinium embonate) Chemical Structure

Cas No.:3546-41-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥540.00
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10mg
¥491.00
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50mg
¥884.00
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100mg
¥1,384.00
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实验参考方法

Cell experiment:

Pyrvinium pamoate is dissolved in DMSO at a concentration of 1 μM and is stocked in aliquots at -20°C. Cells (1×104) are suspended in 200 μL culture medium and then seeded into 96-well plates in quintuplicate overnight. Cells are treated with indicated concentrations of Pyrvinium pamoate (0-8,000 μM). After incubating for 3 days, CCK8 (10 μL) is added into each well and incubated at 37°C for 1 h. The absorbance is measured using a microplate reader at 450 nm[1].

Animal experiment:

Mice: NOD/SCID mice are housed under aseptic conditions in individually ventilated cages. For xenografting, 5×106 Pyrvinium pamoate-pretreated or untreated breast cancer cells (MDA-MB-231) are resuspended in a 1:1 mixture of culture medium and Matrigel and then transplanted into the fourth pair of mammary fat pads of mice (4-6-week-old). After injection, tumor size is measured by calipers each day and tumor growth is plotted. Upon reaching the endpoint, mice are sacrificed and tumors are harvested. All the tumors are formalin-fixed, and paraffin-embedded for hematoxylin and eosin and immunohistochemical staining[1].

References:

[1]. Xu L, et al. WNT pathway inhibitor pyrvinium pamoate inhibits the self-renewal and metastasis of breast cancer stem cells. Int J Oncol. 2016 Mar;48(3):1175-86.
[2]. Wiegering A, et al. The impact of pyrvinium pamoate on colon cancer cell viability. Int J Colorectal Dis. 2014 Oct;29(10):1189-98.
[3]. Venerando A, et al. Pyrvinium pamoate does not activate protein kinase CK1, but promotes Akt/PKB down-regulation and GSK3 activation. Biochem J. 2013 May 15;452(1):131-7.
[4]. Murakoshi M, et al. An anthelmintic drug, pyrvinium pamoate, thwarts fibrosis and ameliorates myocardial contractile dysfunction in a mouse model of myocardial infarction. PLoS One. 2013 Nov 4;8(11):e79374.

产品描述

Pyrvinium is an anthelmintic and anticancer agent.1,2 Dietary administration of pyrvinium reduces worm burden in mouse models of N. dubius, S. obvelata, or A. tetraptera infection (EC50s = 292, 4, and 17 ppm, respectively) but is lethal to mice at higher concentrations (LC50 = 600 ppm).1 Pyrvinium (1 μg/ml) induces cytotoxicity in PANC-1 cells cultured in glucose-deficient medium but not serum- or amino acid-deficient medium or complete medium.2 It reduces tumor growth in a PANC-1 mouse xenograft model when administered at a dose of 100 μg/mouse per day. Pyrvinium (10 nM) also binds to and activates casein kinase 1α (CK1α).3 It inhibits Wnt signaling (EC50 = ~10 nM in a reporter assay) in a CK1α-dependent manner. Formulations containing pyrvinium were previously used in the treatment of pinworm infections.

1.Brody, G.L., and Elward, T.E.Comparative activity of 29 known anthelmintics under standardized drug-diet and gavage medication regimens against four helminth species in miceJ. Parasitol.57(5)1068-1077(1971) 2.Esumi, H., Lu, J., Kurashima, Y., et al.Antitumor activity of pyrvinium pamoate, 6-(dimethylamino)-2-[2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methyl-quinolinium pamoate salt, showing preferential cytotoxicity during glucose starvationCancer Sci.95(8)685-690(2004) 3.Van Acker, H.H., Capsomidis, A., Smits, E.L., et al.CD56 in the immune system: More than a marker for cytotoxicity?Front. Immunol.8892(2017)

Chemical Properties

Cas No. 3546-41-6 SDF
别名 扑蛲灵,Pyrvinium embonate
Canonical SMILES C[N+]1=C2C=CC(N(C)C)=CC2=CC=C1/C=C/C3=C(C)N(C4=CC=CC=C4)C(C)=C3.C[N+]5=C6C=CC(N(C)C)=CC6=CC=C5/C=C/C7=C(C)N(C8=CC=CC=C8)C(C)=C7.O=C(C9=C(O)C(CC%10=C%11C=CC=CC%11=CC(C([O-])=O)=C%10O)=C%12C=CC=CC%12=C9)[O-]
分子式 C26H28N3 . 1/2 C23H14O6 分子量 575.7
溶解度 DMSO : ≥ 24 mg/mL (41.69 mM) 储存条件 4°C, protect from light ,unstable in solution, ready to use.
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1 mM 1.737 mL 8.6851 mL 17.3702 mL
5 mM 0.3474 mL 1.737 mL 3.474 mL
10 mM 0.1737 mL 0.8685 mL 1.737 mL
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Research Update

The Diagnosis and Treatment of Pinworm Infection

Dtsch Arztebl Int 2019 Mar 29;116(13):213-219.PMID:31064642DOI:10.3238/arztebl.2019.0213.

Background: Symptomatic infection with pinworm (Enterobius vermicularis), a human pathogen, is clinically relevant in Germany, with an estimated prevalence in childhood of 2-20%. Enterobiasis can cause major mental distress. There is little systematically verified knowledge on the treatment of this condition, and there is no corresponding German guideline. This review is, therefore, intended as a summary of the current state of knowledge. Methods: This review is based on pertinent publications retrieved by a selective search in PubMed for literature appearing from 1 January 1990 to 5 February 2019 and containing the search terms "enterobiasis," "oxyuriasis," "Enterobius vermicula- ris," "pinworm," and "threadworm." Results: More than one billion people worldwide are thought to be infected with pinworm. Estimates of its prevalence among kindergarten and primary-school pupils in Europe are generally near 20%. Infants (<2 years of age), adolescents (>14 years of age), and adults are only sporadically affected. The main risk factors are age 4-11 years, uncontrolled anus-finger-mouth contact, nail-biting (onychophagia/peri- onychophagia), unsupervised body hygiene, and poor compliance with basic hand hygiene. No large-scale, randomized, controlled trials of treatment are available. The approved antihelminthic agents are mebendazole, pyrantel embonate, and Pyrvinium embonate (success rates up to >90%). For recurrent infections, prolonged treatment for up to 16 weeks (a "pulse scheme") is recommended. Conclusion: In nearly all cases, antihelminthic treatment along with attention to hygienic measures can successfully eradicate pinworm infection and prevent recurrence and autoinfection. The involvement of all persons living in the patient's house- hold, including sexual partners, is a prerequisite to the lasting success of treatment.