Carbosulfan
(Synonyms: 丁硫克百威) 目录号 : GC32257
Carbosulfan强效抑制CYP3A4,适度抑制CYP1A1/2和CYP2C19。
Cas No.:55285-14-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
[1]. Abass K, et al. Metabolism of carbosulfan II. Human interindividual variability in its in vitro hepatic biotransformation and the identification of the cytochrome P450 isoforms involved. Chem Biol Interact. 2010 May 14;185(3):163-173.
| Cas No. | 55285-14-8 | SDF | |
| 别名 | 丁硫克百威 | ||
| Canonical SMILES | O=C(OC1=C(OC(C)(C)C2)C2=CC=C1)N(SN(CCCC)CCCC)C | ||
| 分子式 | C20H32N2O3S | 分子量 | 380.54 |
| 溶解度 | DMSO : ≥ 68 mg/mL (178.69 mM) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6278 mL | 13.1392 mL | 26.2784 mL |
| 5 mM | 0.5256 mL | 2.6278 mL | 5.2557 mL |
| 10 mM | 0.2628 mL | 1.3139 mL | 2.6278 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。
Quantitative determination of Carbosulfan residues by surface-enhanced Raman spectroscopy
Spectrochim Acta A Mol Biomol Spectrosc 2023 Apr 5;290:122315.PMID:36621079DOI:10.1016/j.saa.2022.122315.
Carbosulfan gets easily decomposed into carbofuran and 3-Hydroxy carbofuran in vegetables and forms harmful residues. To detect the residues of Carbosulfan in vegetables (for example, cowpeas), a super-sensitive method of surface-enhanced Raman spectroscopy (SERS) was used in this work. Silver sol was prepared as the SERS substrate. To solve the adsorption problem of Carbosulfan on Ag nanoparticles, 2, 6-dichloroquinone-4-chlorimide (chromogenic agent), and sodium hydroxide were added in Carbosulfan to generate a complex, which was then mixed with the silver sol in the best proportion to examine SERS spectra. According to density functional theory calculations, the spectral peak positions of Carbosulfan were determined. The optimal mixing ratio of the complex and the silver sol to obtain the optimal SERS spectrum and the detection limit of Carbosulfan were investigated. The ultra-sensitive detection of Carbosulfan residues (8.7 脳 10-11 g/L) in cowpeas was realized. The results of this work indicate that SERS is a promising technique for detecting single-molecule pesticide residues in vegetables.
Bioaccumulation and Metabolism of Carbosulfan in Zebrafish ( Danio rerio) and the Toxic Effects of Its Metabolites
J Agric Food Chem 2019 Nov 13;67(45):12348-12356.PMID:31638788DOI:10.1021/acs.jafc.9b03674.
Carbosulfan is a carbamate insecticide that has been widely used in agriculture. However, studies showed that Carbosulfan could be highly toxic to aquatic organisms. The metabolism of Carbosulfan in adult zebrafish is still largely unexplored, and the metabolites in individual or in combination may pose a potential threat to zebrafish. In the present study, the bioaccumulation and metabolism of Carbosulfan in zebrafish (Danio rerio) were assessed, and the main metabolites, including carbofuran and 3-hydroxycarbofuran, were determined. The toxicity of Carbosulfan and its metabolites individually or in combination to zebrafish was also investigated. The bioaccumulation and metabolism experiment indicated that Carbosulfan was not highly accumulated in zebrafish, with a bioaccumulation factor of 18 after being exposed to Carbosulfan for 15 days, and the metabolism was fast, with a half-life of 1.63 d. The two main metabolites were relatively persistent, with half-lives of 3.33 and 5.68 d for carbofuran and 3-hydroxycarbofuran, respectively. The acute toxicity assay showed that carbofuran and 3-hydroxycarbofuran had 96-h LC50 values of 0.15 and 0.36 mg/L, showing them to be more toxic than Carbosulfan (96-h LC50 = 0.53 mg/L). Combinations of binary or ternary mixtures of Carbosulfan and its metabolites displayed coincident synergistic effects on acute toxicity, with additive index (AI) values of 1.9-14.3. In the livers and gills of zebrafish exposed to Carbosulfan, carbofuran, and 3-hydroxycarbofuran, activities of catalase, superoxide dismutase, and glutathione-S-transferase were significantly changed in most cases, and the content of malondialdehyde was greatly increased, indicating that Carbosulfan and its metabolites induced varying degrees of oxidative stress. The metabolites were more persistent and toxic to zebrafish and exhibit coincident synergistic effects in combination. These results can provide evidence for the potential risk of pesticides and highlight the importance of a systematic assessment for the combination of the precursor and its metabolites.
Degradation of malathion and Carbosulfan by ozone water and analysis of their by-products
J Sci Food Agric 2022 Dec;102(15):7072-7078.PMID:35690892DOI:10.1002/jsfa.12068.
Background: Treatment by ozone water is an emerging technology for the degradation of pesticide residues in vegetables. The ozone dissolved in water generates hydroxyl radicals (路 OH), which are highly effective in decomposing organic substances, such as malathion and Carbosulfan. Results: We found that washing pak choi with 2.0 mg L-1 ozone water for 30 min resulted in 58.3% and 38.2% degradation of the malathion and Carbosulfan contents respectively, and the degradation rates of these pure pesticides were 83.0% and 66.3% respectively. In addition, the 'first + first'-order reaction kinetic model was found to predict the trend in the pesticide content during ozone water treatment. Based on investigations by gas chromatography-mass spectrometry combined with the structures of the pesticides, the by-products generated were identified. More specifically, the ozonation-based degradation of Carbosulfan generated carbofuran and benzofuranol, whereas malathion produced succinic acid and phosphoric acid. Although some new harmful compounds were formed during degradation of the parent pesticides, these were only present in trace quantities and were transient intermediates that eventually disappeared during the reaction. Conclusion: Our results, therefore, indicate that ozone water treatment technology for pesticide residue degradation is worthy of popularization and application. 漏 2022 Society of Chemical Industry.
Carbosulfan exposure during embryonic period can cause developmental disability in rats
Environ Toxicol Pharmacol 2014 Jul;38(1):230-8.PMID:24973665DOI:10.1016/j.etap.2014.05.009.
Carbosulfan, a wide spectrum pesticide is used to improve crop productivity. During their application, they disperse in the environment exerting harmful consequences on human health. We speculated that exposure to Carbosulfan, a carbamate insecticide during early development can affect neurogenesis and synaptic development. In order to test this, pregnant dams were exposed to Carbosulfan in four doses (0.5, 1, 2, and 4mg/kg) during the embryonic period (ED 1-15). Offspring were evaluated for neurobehavioral changes, oxidative markers, acetylcholinesterase levels, and formation of carbonylated proteins. Histopathology of the cerebellum was carried out. Carbosulfan exposure produced alteration in sensorimotor tasks, motor function and elevated anxiety in pups. Carbosulfan affected growth rate of pups in a dose dependent manner. A significant increase in malondialdehyde, a lipid peroxide marker, carbonylated proteins and a dose dependent decrease in the levels of glutathione and glutathione peroxidase were observed. Carbosulfan produced a decline in acetylcholinesterase levels which might contribute to poor exploratory behavior. Distinct changes in the Purkinje cells were observed as the dose of Carbosulfan increased. Largely, alteration in behavior can be due to oxidative damage, thereby, affecting neurogenesis, synaptogenesis and myelination. Therefore the propensity of Carbosulfan to induce developmental disability is high and should be cautiously avoided during embryonic development.
Residues of Carbosulfan and its metabolites carbofuran and 3-hydroxy carbofuran in rice field ecosystem in China
J Environ Sci Health B 2016;51(6):351-7.PMID:26963425DOI:10.1080/03601234.2015.1120606.
The fate of Carbosulfan (seed treatment dry powder) was studied in rice field ecosystem, and a simple and reliable analytical method was developed for determination of Carbosulfan, carbofuran, and 3-hydroxyl carbofuran in brown rice, rice straw, paddy water, and soil. The target compounds were extracted using acetonitrile or dichloromethane, cleaned up on acidic alumina or florisil solid phase extraction (SPE) cartridge, and analyzed by gas chromatography. The average recoveries of Carbosulfan, carbofuran and 3-hydroxy carbofuran in brown rice, rice straw, paddy water, and soil ranged from 72.71% to 105.07%, with relative standard deviations of 2.00-8.80%. The limits of quantitation (LOQs) of Carbosulfan, carbofuran and 3-hydroxy carbofuran in the samples (brown rice, rice straw, paddy water and soil) were 0.011, 0.0091, 0.014, 0.010 mg kg(-1), 0.016, 0.019, 0.025, 0.013 mg kg(-1), and 0.031, 0.039, 0.035, 0.036 mg kg(-1), respectively. The trials results showed that the half-lives of Carbosulfan, carbofuran and 3-hydroxy carbofuran in rice straw were 4.0, 2.6 days, 3.9, 6.0 days, and 5.8, 7.0 days in Zhejiang and Hunan, respectively. Carbosulfan, carbofuran and 3-hydroxy carbofuran were detected in soils. Carbosulfan and 3-hydroxy carbofuran were almost undetectable in paddy water. Carbofuran was detected in paddy water. The final residues of Carbosulfan, carbofuran and 3-hydroxy carbofuran in brown rice were lower than 0.05 mg kg(-1), which were lower than 0.5 mg kg(-1) (MRL of Carbosulfan) or 0.1 mg kg(-1) (MRL of carbofuran). Therefore, a dosage of 420 g active ingredient per 100 kg seed was recommended, which could be considered as safe to human beings and animals. These would contribute to provide the scientific basis of using this insecticide.