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Thimerosal Sale

(Synonyms: 硫柳汞钠,Sodium ethylmercurithiosalicylate) 目录号 : GC48571

A mercurial antimicrobial agent

Thimerosal Chemical Structure

Cas No.:54-64-8

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产品描述

Thimerosal is a mercurial antimicrobial agent.1,2 It is bacteriostatic against hemolytic streptococci and fungistatic against H. capsulatum, B. dermatitidis, and S. schenckii. Thimerosal (1-250 µM) induces apoptosis in HCN-1A human cortical neurons and various neuroblastoma cells.3,4 In vivo, thimerosal (80 mg/kg, i.p.) induces footpad swelling and dorsal skin contact dermatitis in a mouse model of pseudo-allergic reaction.5 Formulations containing thimerosal have been used as antiseptics and preservatives in vaccines.

1.Morton, H.E., North, L.L., Jr., and Engley, F.B., Jr.The bacteriostatic and bactericidal actions of some mercurial compounds on hemolytic streptococciJ. Am. Med. Assoc.136(1)37-41(1948) 2.Deighton, F.J., Hall, N.K., and Larsh, H.W.Merthiolate treatment of pathogenic fungiJ. Clin. Microbiol.10(2)144-146(1979) 3.Baskin, D.S., Ngo, H., and Didenko, V.V.Thimerosal induces DNA breaks, caspase-3 activation, membrane damage, and cell death in cultured human neurons and fibroblastsToxicol. Sci.74361-368(2003) 4.DÓrea, J.G.Integrating experimental (in vitro and in vivo) neurotoxicity studies of low-dose thimerosal relevant to vaccinesNeurochem. Res.36(3)927-038(2011) 5.Peng, B., Che, D., Hao, Y., et al.Thimerosal induces skin pseudo-allergic reaction via Mas-related G-protein coupled receptor B2J. Dermatol. Sci.95(3)99-106(2019)

Chemical Properties

Cas No. 54-64-8 SDF
别名 硫柳汞钠,Sodium ethylmercurithiosalicylate
Canonical SMILES O=C([O-])C1=CC=CC=C1[S][Hg]CC.[Na+]
分子式 C9H9HgO2S•Na 分子量 404.8
溶解度 Ethanol: soluble,Water: soluble 储存条件 Store at -20°C, protect from light
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1 mg 5 mg 10 mg
1 mM 2.4704 mL 12.3518 mL 24.7036 mL
5 mM 0.4941 mL 2.4704 mL 4.9407 mL
10 mM 0.247 mL 1.2352 mL 2.4704 mL
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Research Update

Thimerosal: clinical, epidemiologic and biochemical studies

Clin Chim Acta 2015 Apr 15;444:212-20.PMID:25708367DOI:10.1016/j.cca.2015.02.030.

Introduction: Thimerosal (or Thiomersal) is a trade name for an organomercurial compound (sodium ethyl-mercury (Hg) thiosalicylate) that is 49.55% Hg by weight, which rapidly decomposes in aqueous saline solutions into ethyl-Hg hydroxide and ethyl-Hg chloride. Developed in 1927, it has been and is still being used as a preservative in some cosmetics, topical pharmaceuticals, and biological drug products, including vaccines. Concerns have been voiced about its use because it is toxic to human cells. Although it is banned in several countries, it continues to be added to some vaccines in the United States and many vaccines in the developing world. Discussion: This critical review focuses on the clinical, epidemiological, and biochemical studies of adverse effects from Thimerosal in developing humans. This review will include research that examines fetal, infant, and childhood death; birth defects; neurodevelopmental testing deficits in children; and neurodevelopmental disorders (attention deficit/hyperactivity disorder, autism spectrum disorder, tic disorder, and specific developmental delays). The review will also look at the research that examined the outcomes of acute accidental ethyl-Hg poisoning in humans. The studies that examine the underlying biochemical insights into the neuronal cellular damage will also be explored. Conclusion: The culmination of the research that examines the effects of Thimerosal in humans indicates that it is a poison at minute levels with a plethora of deleterious consequences, even at the levels currently administered in vaccines.

Thimerosal as discrimination: vaccine disparity in the UN Minamata Convention on mercury

Indian J Med Ethics 2014 Oct-Dec;11(4):206-18.PMID:25101548DOI:10.20529/IJME.2014.054.

When addressing toxins, one unmistakable parallel exists between biology and politics: developing children and developing nations are those most vulnerable to toxic exposures. This disturbing parallel is the subject of this critical review, which examines the use and distribution of the mercury (Hg)-based compound, Thimerosal, in vaccines. Developed in 1927, Thimerosal is 49.55% Hg by weight and breaks down in the body into ethyl-Hg chloride, ethyl-Hg hydroxide and sodium thiosalicylate. Since the early 1930s, there has been evidence indicating that Thimerosal poses a hazard to the health of human beings and is ineffective as an antimicrobial agent. While children in the developed and predominantly western nations receive doses of mostly no-thimerosal and reduced-thimerosal vaccines, children in the developing nations receive many doses of several unreduced thimerosal-containing vaccines (TCVs). Thus, Thimerosal has continued to be a part of the global vaccine supply and its acceptability as a component of vaccine formulations remained unchallenged until 2010, when the United Nations (UN), through the UN Environment Programme, began negotiations to write the global, legally binding Minamata Convention on Hg. During the negotiations, TCVs were dropped from the list of Hg-containing products to be regulated. Consequently, a double standard in vaccine safety, which previously existed due to ignorance and economic reasons, has now been institutionalised as global policy. Ultimately, the Minamata Convention on Hg has sanctioned the inequitable distribution of Thimerosal by specifically exempting TCVs from regulation, condoning a two-tier standard of vaccine safety: a predominantly no-thimerosal and reduced-thimerosal standard for developed nations and a predominantly thimerosal-containing one for developing nations. This disparity must now be evaluated urgently as a potential form of institutionalised discrimination.

Low-dose Thimerosal (ethyl-mercury) is still used in infants` vaccines: Should we be concerned with this form of exposure?

J Trace Elem Med Biol 2018 Sep;49:134-139.PMID:29895363DOI:10.1016/j.jtemb.2018.05.010.

In developing countries, Thimerosal-containing vaccines (TCV) are the main causes of organic Hg exposure for newborns, neonates, and infants immunized with TCV. This article addresses early-life exposure to this unique organic mercury compound (ethylmercury-EtHg) and the risks of its exposure. English language studies pertaining to Thimerosal/EtHg toxicity and exposure during early life were searched in PubMed; and, those publications judged to be relevant to the topic of this review were selected. The risk from the neurotoxic effects of pre- and post-natal Hg exposures depend, in part, on aggravating or attenuating environmental and/or genetic-associated factors. Health authorities in charge of controlling infectious disease dismiss the toxicology of mercury (immunological and subtle neurological effects as insignificant) related to low-dose Thimerosal. The review addresses the evidence that brings into question the safety of Thimerosal that is still present in vaccines given to pregnant women, infants, and children in developing countries, and recognizes the ethical imperative to extend the use of Thimerosal-free vaccines to developing countries, not just developed countries.

Low-dose Thimerosal in pediatric vaccines: Adverse effects in perspective

Environ Res 2017 Jan;152:280-293.PMID:27816865DOI:10.1016/j.envres.2016.10.028.

Vaccines are prophylactics used as the first line of intervention to prevent, control and eradicate infectious diseases. Young children (before the age of six months) are the demographic group most exposed to recommended/mandatory vaccines preserved with Thimerosal and its metabolite ethylmercury (EtHg). Particularly in the less-developed countries, newborns, neonates, and young children are exposed to EtHg because it is still in several of their pediatric vaccines and mothers are often immunized with Thimerosal-containing vaccines (TCVs) during pregnancy. While the immunogenic component of the product has undergone more rigorous testing, Thimerosal, known to have neurotoxic effects even at low doses, has not been scrutinized for the limit of tolerance alone or in combination with adjuvant-Al during immaturity or developmental periods (pregnant women, newborns, infants, and young children). Scientific evidence has shown the potential hazards of Thimerosal in experiments that modeled vaccine-EtHg concentrations. Observational population studies have revealed uncertainties related to neurological effects. However, consistently, they showed a link of EtHg with risk of certain neurodevelopment disorders, such as tic disorder, while clearly revealing the benefits of removing Thimerosal from children's vaccines (associated with immunological reactions) in developed countries. So far, only rich countries have benefited from withdrawing the risk of exposing young children to EtHg. Regarding Thimerosal administered to the very young, we have sufficient studies that characterize a state of uncertainty: the collective evidence strongly suggests that Thimerosal exposure is associated with adverse neurodevelopmental outcomes. It is claimed that the continued use of Thimerosal in the less-developed countries is due to the cost to change to another preservative, such as 2-phenoxyethanol. However, the estimated cost increase per child in the first year of life is lower than estimated lifetime cost of caring for a child with a neurodevelopmental disorder, such tic disorder. The evidence indicates that Thimerosal-free vaccine options should be made available in developing countries.

Thimerosal: a versatile sulfhydryl reagent, calcium mobilizer, and cell function-modulating agent

Gen Pharmacol 1999 Jul;33(1):1-6.PMID:10428009DOI:10.1016/s0306-3623(98)00258-4.

An overview of the literature concerning the effects of Thimerosal is presented. Because of its antibacterial effect, Thimerosal is used for a variety of practical purposes such as antiseptic and preservative. In biomedical studies, Thimerosal is used as a sulfhydryl reagent, and as a calcium-mobilizing agent. The ability of Thimerosal to act as a sulfhydryl group is related to the presence of mercury. Relatively little study has been devoted to the mechanism of the reaction of Thimerosal with the sulfhydryl group; the sulfhydryl reactive capacity is mostly concluded on the basis of inactivation of the effect by dithiothreitol (DTT). Thimersal causes a release of calcium from intracellular stores in many cells types; this is followed by an influx of extracellular calcium. Both InsP3- and ryanodine-sensitive calcium stores may be affected. Studies with permeabilized cells or organelles show that the effect of Thimerosal on calcium is dependent on the concentration: low concentrations of Thimerosal stimulate calcium release, high concentrations are inhibitory. This dependence is not found in intact cells. Thimerosal may activate or inhibit a number of cell functions. These are often related to the ability to release calcium or with the sulfhydryl reactivity. In platelets, Thimerosal causes aggregation, increase of arachidonic acid metabolism, and exocytotic release of serotonin. In neutrophils, Thimerosal causes, besides an increase of cytosolic free calcium, an increase of formyl-methionyl-leucyl-phenylalanine (fMLP)-activated leukotriene release, and a modulation of chemotactic migration and exocytosis. At low concentrations, Thimerosal induces chemotactic migration of neutrophils, in the absence of other chemoattractants. The effect is also observed with thiosalicylic acid, indicating that the stimulation of migration was due to the thiosalicylic acid moiety of the Thimerosal molecule. At higher concentrations, Thimerosal causes inhibition of fMLP-activated migration. Low concentrations of Thimerosal, but not of thiosalicylic acid, induced exocytotic enzyme release from neutrophils. High concentrations of Thimerosal inhibited fMLP-activated exocytosis. The results point to an involvement of calcium mobilization and calcium influx of activation, and reaction with sulfhydryl groups for inhibition.