DTPA
(Synonyms: 二乙烯三胺五醋酸,Diethylenetriaminepentaacetic acid; DTPA) 目录号 : GC49058
A cell-impermeable metal chelating agent
Cas No.:67-43-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
DTPA is a cell-impermeable metal chelating agent.1,2 It chelates copper, iron, zinc, and manganese, as well as calcium, magnesium, and plutonium.1,3 DTPA has been used as a metal chelating agent in the study of ferroptosis.4 It reduces the skeletal plutonium burden and incidence of bone tumors, as well as increases survival in a mouse model of intravenous plutonium exposure when administered at a dose of 500 mg/kg.3 Formulations containing DTPA conjugated to radioactive compounds have been used as diagnostic agents for brain imaging, renal visualization, and lung imaging.
1.Arts, J., Bade, S., Badrinas, M., et al.Should DTPA, an Aminocarboxylic acid (ethylenediamine-based) chelating agent, be considered a developmental toxicant•Regul. Toxicol. Pharmacol.97197-208(2018) 2.Killilea, D.W., Atamna, H., Liao, C., et al.Iron accumulation during cellular senescence in human fibroblasts in vitroAntioxid. Redox Signal.5(5)507-516(2003) 3.Osenthal, M.W., and Lindenbaum, A.Influence of DTPA therapy on long-term effects of retained monomeric plutonium: Comparison with polymeric plutoniumRadiat. Res.31(3)506-521(1967) 4.Wenzel, S.E., Tyurina, Y.Y., Zhao, J., et al.PEBP1 wardens ferroptosis by enabling lipoxygenase generation of lipid death signalsCell171(3)628-641(2017)
| Cas No. | 67-43-6 | SDF | |
| 别名 | 二乙烯三胺五醋酸,Diethylenetriaminepentaacetic acid; DTPA | ||
| Canonical SMILES | O=C(CN(CCN(CCN(CC(O)=O)CC(O)=O)CC(O)=O)CC(O)=O)O | ||
| 分子式 | C14H23N3O10 | 分子量 | 393.4 |
| 溶解度 | Ethanol: slightly soluble,Methanol: slightly soluble,PBS (pH 7.2): slightly soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5419 mL | 12.7097 mL | 25.4194 mL |
| 5 mM | 0.5084 mL | 2.5419 mL | 5.0839 mL |
| 10 mM | 0.2542 mL | 1.271 mL | 2.5419 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Should DTPA, an Aminocarboxylic acid (ethylenediamine-based) chelating agent, be considered a developmental toxicant?
Regul Toxicol Pharmacol 2018 Aug;97:197-208.PMID:29964121DOI:10.1016/j.yrtph.2018.06.019.
Aminocarboxylic acid (ethylenediamine-based) chelating agents, such as DTPA and EDTA, are widely used in a variety of products and processes. Recently the European RAC proposed to classify DTPA as a developmental toxicant Category 1B according to CLP. This paper provides unequivocal and significant evidence that developmental effects cannot be considered an intrinsic property of the chelating substances themselves since: (1) animals fed a zinc deficient diet during gestation exhibit developmental toxicity of a similar nature and severity to that observed in studies involving such chelates, (2) sufficient supplementation of zinc in the diet, or administration of zinc bound chelates, completely negates the developmental effects. Moreover, the bioavailability of DTPA is very low with >95% of oral doses excreted unchanged via the feces within 24 h. If DTPA would possess the intrinsic property to be developmentally toxic, simple zinc supplementation should not be sufficient to negate these effects. Furthermore, the relevance of classification is highly questionable since worker or consumer exposure could not lead to a scenario whereby sufficient zinc deficiency would manifest itself. Therefore classification of DTPA for such effects is not protective of human health; instead it leads to onerous and disproportionate restrictions being placed on this substance.
Environmental fate of EDTA and DTPA
Rev Environ Contam Toxicol 1997;152:85-111.PMID:9297986DOI:10.1007/978-1-4612-1964-4_3.
EDTA can be extremely persistent in WWTP and also in natural waters; DTPA seems more biodegradable. However, the biodegradability of DTPA might be of negligible significance as EDTA, and in some cases also DTPA, are generally found in the receiving waters of many industrial areas, thus being classified as one of the major organic pollutants discharged in waters. The photochemical degradation of Fe(III) complexes of these compounds is documented, but the extent to which these results can be applied to natural waters is not clear. There exist still some uncertainties in the chemical speciation, adsorption, overall degradation, and ultimately the eutrophication effect of EDTA and especially of DTPA. It can be inferred that EDTA can affect the essential and nonessential metal balance in natural waters as well as in aquatic organisms, even in the long term. The estimation of the chemical speciation of EDTA and DTPA in natural waters is a challenging task because of of the complexicity of the system and should be based not only on equilibrium calculations but also on direct analytical determinations of diverse metal species. Unfortunately, analytical methods for speciation studies at environmentally relevant concentrations are not available. Also, monitoring of EDTA or DTPA in sediments and solid particles has not been initiated. EDTA and DTPA are not expected to be acutely toxic to aquatic organisms. On the other hand, in natural waters, several compounds affect organisms simultaneously. Therefore, EDTA and DTPA can contribute to the aquatic toxicity at significantly lower concentration than those determined by short-term toxicity tests. Also, more studies should be directed to estimating chronic effects, including the possible imbalance of body calcium in animals and other organisms. EDTA and DTPA can certainly desorb heavy metals bound to sediments and also prevent heavy metal sedimentation, thus increasing their cycle in water. However, these metal complexes are not expected to be as bioavailable as a free metal ions. Taken together, EDTA and DTPA, being persistent compounds, contribute to the general chemicalization of the aquatic environment. They can also cause several indirect and, under extreme circumstances, direct effects in the aquatic environment. Thus, their release into natural waters should be minimized wherever possible.
Calcium and zinc DTPA administration for internal contamination with plutonium-238 and americium-241
Curr Pharm Biotechnol 2012 Aug;13(10):1957-63.PMID:22352730DOI:10.2174/138920112802273308.
The accidental or intentional release of plutonium or americium can cause acute and long term adverse health effects if they enter the human body by ingestion, inhalation, or injection. These effects can be prevented by rapid removal of these radionuclides by chelators such as calcium or zinc diethylenetriaminepentaacetate (calcium or zinc DTPA). These compounds have been shown to be efficacious in enhancing the elimination of members of the actinide family particularly plutonium and americium when administered intravenously or by nebulizer. The efficacy and adverse effects profile depend on several factors that include the route of internalization of the actinide, the type, and route time of administration of the chelator, and whether the calcium or zinc salt of DTPA is used. Current and future research efforts should be directed at overcoming limitations associated with the use of these complex drugs by using innovative methods that can enhance their structural and therapeutic properties.
Delivery of DTPA through Liposomes as a Good Strategy for Enhancing Plutonium Decorporation Regardless of Treatment Regimen
Radiat Res 2018 May;189(5):477-489.PMID:29528770DOI:10.1667/RR14968.1.
In this study, we assessed the efficacy of unilamellar 110-nm liposomes encapsulating the chelating agent diethylenetriaminepentaacetic acid (DTPA) in plutonium-exposed rats. Rats were contaminated by intravenous administration of the soluble citrate form of plutonium. The comparative effects of liposomal and free DTPA at similar doses were examined in terms of limitation of alpha activity burden in rats receiving various treatment regimens. Liposomal DTPA given at 1 h after contamination more significantly prevented the accumulation of plutonium in tissues than did free DTPA. Also, when compared to free DTPA, liposome-entrapped DTPA was more efficient when given at late times for mobilization of deposited plutonium. In addition, repeated injections of liposomal DTPA further improved the removal of plutonium compared to single injection. Various possible mechanisms of action for DTPA delivered through liposomes are discussed. The advantage of liposomal DTPA over free DTPA was undoubtedly directly and indirectly due to the better cell penetration of DTPA when loaded within liposomes, mainly in the tissues of the mononuclear phagocytic system. The decorporation induced by liposomal DTPA may result first from intracellular chelation of plutonium deposited in soft tissues, predominantly in the liver. Afterwards, the slow release of free DTPA molecules from these same tissues may enable a sustained action of DTPA, probably mainly by extracellular chelation of plutonium available on bone surfaces. In conclusion, decorporation of plutonium can be significantly improved by liposomal encapsulation of DTPA regardless of the treatment regimen applied.
Species-dependent effective concentration of DTPA in plasma for chelation of 241Am
Health Phys 2013 Aug;105(2):208-14.PMID:23799506DOI:10.1097/HP.0b013e318290ca33.
Diethylenetriaminepentaacetic acid (DTPA) is a chelating agent that is used to facilitate the elimination of radionuclides such as americium from contaminated individuals. Its primary site of action is in the blood, where it competes with various biological ligands, including transferrin and albumin, for the binding of radioactive metals. To evaluate the chelation potential of DTPA under these conditions, the competitive binding of Am between DTPA and plasma proteins was studied in rat, beagle, and human plasma in vitro. Following incubation of DTPA and Am in plasma, the Am-bound ligands were fractionated by ultrafiltration and ion-exchange chromatography, and each fraction was assayed for Am content by gamma scintillation counting. Dose response curves of DTPA for Am binding were established, and these models were used to calculate the 90% maximal effective concentration, or EC90, of DTPA in each plasma system. The EC90 were determined to be 31.4, 15.9, and 10.0 μM in rat, beagle, and human plasma, respectively. These values correspond to plasma concentrations of DTPA that maximize Am chelation while minimizing excess DTPA. Based on the pharmacokinetic profile of DTPA in humans, after a standard 30 μmol kg intravenous bolus injection, the plasma concentration of DTPA remains above EC90 for approximately 5.6 h. Likewise, the effective duration of DTPA in rat and beagle were determined to be 0.67 and 1.7 h, respectively. These results suggest that species differences must be considered when translating DTPA efficacy data from animals to humans and offer further insights into improving the current DTPA treatment regimen.