Bromadiolone
(Synonyms: Bromatrol, Broprodifacoum) 目录号 : GC45620
An anticoagulant rodenticide
Cas No.:28772-56-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bromadiolone is a second generation anticoagulant rodenticide and 4-hydroxycoumarin derivative.1,2 It is an inhibitor of vitamin K epoxide reductase (VKOR) that inhibits blood clotting. It inhibits human VKOR complex subunit 1 (VKORC1) with an IC50 value of 1.6 nM in a cell-based assay.3 Bromadiolone is toxic to rodents, including mice (LD50 = 1.75 mg/kg) and rats (LD50s = 1.05 and 1.83 mg/kg for males and females, respectively).4,5 It does not significantly affect breeding performance in mice when administered at a dose of up to 70% of the LD50 value.6 Resistance to bromadiolone is conferred by mutations to the VKOR gene, Vkorc1.7 Formulations containing bromadiolone have been used in the control of rodent pest populations.
|1. Watt, B.E., Proudfoot, A.T., Bradberry, S.M., et al. Anticoagulant rodenticides. Toxicol. Rev. 24(4), 259-269 (2005).|2. Misenheimer, T.M., Lund, M., Baker, A.E.M., et al. Biochemical basis of warfarin and bromadiolone resistance in the house mouse, Mus musculus domesticus. Biochem. Pharmacol. 47(4), 673-678 (1994).|3. Czogalla, K.J., Liphardt, K., H•ning, K., et al. VKORC1 and VKORC1L1 have distinctly different oral anticoagulant dose-response characteristics and binding sites. Blood Adv. 2(6), 691-702 (2018).|4. Vandenbroucke, V., Bousquet-Melou, A., De Backer, P., et al. Pharmacokinetics of eight anticoagulant rodenticides in mice after single oral administration. J. Vet. Pharmacol. Ther. 31(5), 437-445 (2008).|5. Garg, N., and Singla, N. Toxicity of second generation anticoagulant bromadiolone against Rattus Rattus: individual and sex specific variations. Cibtech J. Zoo. 3(2), 43-48 (2014).|6. Twigg, L.E., and Kay, B.J. The effect of sub-lethal doses of bromadiolone on the breeding performance of house mice (Mus domesticus). Comp. Biochem. Physiol. 110(1), 77-82 (1995).|7. Pelz, H.-J., Rost, S., HÜnerberg, M., et al. The genetic basis of resistance to anticoagulants in rodents. Genetics 170(4), 1839-1847 (2005).
| Cas No. | 28772-56-7 | SDF | |
| 别名 | Bromatrol, Broprodifacoum | ||
| Canonical SMILES | BrC1=CC=C(C2=CC=C(C(O)CC(C3=CC=CC=C3)C4=C(O)C5=C(C=CC=C5)OC4=O)C=C2)C=C1 | ||
| 分子式 | C30H23BrO4 | 分子量 | 527.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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 | 1.8961 mL | 9.4805 mL | 18.9609 mL |
| 5 mM | 0.3792 mL | 1.8961 mL | 3.7922 mL |
| 10 mM | 0.1896 mL | 0.948 mL | 1.8961 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。
Weasel exposure to the anticoagulant rodenticide Bromadiolone in agrarian landscapes of southwestern Europe
Sci Total Environ 2022 Sep 10;838(Pt 1):155914.PMID:35569667DOI:10.1016/j.scitotenv.2022.155914.
Bromadiolone is an anticoagulant rodenticide (AR) commonly used as a plant protection product (PPP) against rodent pests in agricultural lands. ARs can be transferred trophically to predators/scavengers when they consume intoxicated live or dead rodents. ARs exposure in weasels Mustela nivalis, small mustelids specialized on rodent predation, is poorly known in southern Europe. Moreover, in this species there is no information on bioaccumulation of AR diastereomers e.g., cis- and trans-bromadiolone. Trans-bromadiolone is more persistent in the rodent liver and thus, is expected to have a greater probability of trophic transfer to predators. Here, we report on Bromadiolone occurrence, total concentrations and diastereomers proportions (trans- and cis-bromadiolone) in weasels from Castilla y León (north-western Spain) collected in 2010-2017, where Bromadiolone was irregularly applied to control outbreaks of common voles Microtus arvalis mainly with cereal grain bait distributed by the regional government. We also tested variables possibly associated with Bromadiolone occurrence and concentration, such as individual features (e.g., sex), spatio-temporal variables (e.g., year), and exposure risk (e.g., vole outbreaks). Overall Bromadiolone occurrence in weasels was 22% (n = 32, arithmetic mean of concentration of Bromadiolone positives = 0.072 mg/kg). An individual showed signs of Bromadiolone intoxication (i.e., evidence of macroscopic hemorrhages or hyperaemia and hepatic Bromadiolone concentration > 0.1 mg/kg). All the exposed weasels (n = 7) showed only trans-bromadiolone diastereomer in liver, whilst a single analyzed bait from those applied in Castilla y León contained trans- and cis-bromadiolone at 65/35%. Bromadiolone occurrence and concentration in weasels varied yearly. Occurrence was higher in 2012 (100% of weasels), when Bromadiolone was widely distributed, compared to 2016-2017 (2016: 20%; 2017: 8.33%) when Bromadiolone was exceptionally permitted. The highest concentrations happened in 2014 and 2017, both years with vole outbreaks. Our findings indicate that specialist rodent predators could be exposed to Bromadiolone in areas and periods with Bromadiolone treatments against vole outbreaks.
Acute toxic encephalopathy following Bromadiolone intoxication: a case report
BMC Neurol 2021 Jan 7;21(1):8.PMID:33407227DOI:10.1186/s12883-020-02034-2.
Background: Clinically, Bromadiolone poisoning is characterized by severe bleeding complications in various organs and tissues. Bromadiolone-induced toxic encephalopathy is extremely rare. Here, we report a special case of bromadiolone-induced reversible toxic encephalopathy in a patient who had symmetrical lesions in the deep white matter. Case presentation: A 23-year-old woman mainly presented with dizziness, fatigue, alalia and unsteady gait after the ingestion of Bromadiolone. The laboratory examinations showed normal coagulation levels. Brain magnetic resonance imaging (MRI) showed apparent diffusion restriction in the bilateral deep white matter. The clinical manifestations and MRI alterations were reversible within one month of treatment with vitamin K. The neuropsychological assessment showed no neurodegenerative changes at the 2-year follow-up. Conclusion: With the increased use of Bromadiolone as a rodenticide, more cases of ingestion have been reported annually over the past several years. Bromadiolone-induced toxic encephalopathy has no special clinical manifestations and is potentially reversible with timely treatment. Because of the reversible restricted diffusion on diffusion-weighted images (DWI) and low apparent diffusion coefficient (ADC) values, transient intramyelinic cytotoxic oedema is thought to be the cause rather than persistent ischaemia. The underlying pathophysiological mechanism is still unknown and may be coagulant-independent. This clinical case extends the current knowledge about neurotoxicity in cases of Bromadiolone poisoning and indicates that MRI is useful for the early detection of bromadiolone-induced toxic encephalopathy.
Temporal Persistence of Bromadiolone in Decomposing Bodies of Common Kestrel ( Falco tinnunculus)
Toxics 2020 Nov 7;8(4):98.PMID:33171863DOI:10.3390/toxics8040098.
Bromadiolone is a second generation anticoagulant rodenticide (SGAR) used to control pest rodents worldwide. SGARs are frequently involved in secondary poisoning in rodent predators due to their persistence and toxicity. This study aims to evaluate the persistence of Bromadiolone in liver at different stages of carcass decomposition in experimentally-dosed common kestrels (Falco tinnunculus) to understand the possibility of detecting Bromadiolone in cases of wildlife poisoning and the potential risk of tertiary poisoning. Twelve individuals were divided into the bromadiolone-dose group (dosed with 55 mg/kg b.w) and the control group. Hepatic Bromadiolone concentrations found in each stage of decomposition were: 3000, 2891, 4804, 4245, 8848, and 756 ng/g dry weight at 1-2 h (fresh carcass), 24 h (moderate decomposition), 72 h, 96 h (advanced decomposition), seven days (very advanced decomposition), and 15 days (initial skeletal reduction) after death, respectively. Liver Bromadiolone concentrations in carcasses remained relatively stable over the first four days and raised on day 7 of decomposition under the specific conditions of this experiment, presenting a risk of causing tertiary poisoning. However, at the initial skeletal reduction stage, liver Bromadiolone concentration declined, which should be considered to interpret toxicological analyses and for proper diagnosis. This experimental study provides for the first time some light to better understand the degradation of SGARs in carcasses in the wild.
Reversible leukoencephalopathy caused by 2 rodenticides Bromadiolone and fluoroacetamide: A case report and literature review
Medicine (Baltimore) 2021 Mar 5;100(9):e25053.PMID:33655984DOI:10.1097/MD.0000000000025053.
Rationale: With the easy access, rodenticide poisoning has been a public health problem in many countries. Characteristics of central nervous system (CNS) lesions induced by rodenticides are scarcely reported. Patient concerns: We presented a case of a 40-year-old man with seizure and consciousness disorder, coagulation dysfunction, and symmetric lesions in white matter and corpus callosum. Diagnosis: He was diagnosed with rodenticide poisoning due to Bromadiolone and fluoroacetamide. Interventions: He was treated with vitamin K, hemoperfusion, acetamide, and calcium gluconate. Outcomes: His leukoencephalopathy was reversed rapidly with the improvement of clinical symptoms. Lessons: This report presented the impact of rodenticide poisoning on CNS and the dynamic changes of brain lesions, and highlighted the importance of timely targeted treatments.
Cis-bromadiolone diastereoisomer is not involved in Bromadiolone Red Kite (Milvus milvus) poisoning
Sci Total Environ 2017 Dec 1;601-602:1412-1417.PMID:28605859DOI:10.1016/j.scitotenv.2017.06.011.
Anticoagulant rodenticides (ARs) are widely used pesticides to control rodent populations. Bromadiolone, a second generation anticoagulant rodenticide (SGARs), is authorized in France to control the population of water voles (Arvicola scherman). The persistence of SGARs in rodents is responsible for secondary exposure or poisoning of predators and scavengers, and is of ecological concern for the conservation of endangered species. Commercial formulations are a mixture of two diastereoisomers of Bromadiolone: 70-90% is trans-bromadiolone and 10-30% is cis-bromadiolone. Both diastereoisomers have been shown to inhibit coagulation function with the same potency. On the other hand, cis-bromadiolone has been shown to be less tissue-persistent than trans-bromadiolone in rats. This difference led to residue levels in rats with substantially weakened proportion in cis-bromadiolone compared to the composition of baits. In this study, a multi-residue LC-MS/MS method for the quantification of the diastereoisomers of SGARs was used to investigate their proportions in field samples of predators. In 2011, 28 red kites (Milvus milvus) were found dead within a few months of Bromadiolone application in grassland to control water vole outbreaks. In this study, we report the concentrations of the two diastereoisomers of Bromadiolone measured in the livers of thirteen red kites. Exposure to Bromadiolone was apparent in all the kites with hepatic concentrations of trans-bromadiolone ranging from 390 to 870ng/g (89 to 99% of summed SGARs). However, cis-bromadiolone was not detected in 5 of 13 red kites and was present at very low concentrations (below 2.2ng/g) in 8 of 13 kites, demonstrating that cis-bromadiolone is not involved in this red kite poisoning event. The results suggest that a change of the proportions of Bromadiolone diastereoisomers in baits could reduce the risk of secondary poisoning of predators, but retain primary toxicity for control rodent outbreaks.