Furosemide-d5
(Synonyms: 呋塞米 D5) 目录号 : GC47385
An internal standard for the quantification of furosemide
Cas No.:1189482-35-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Furosemide-d5 is intended for use as an internal standard for the quantification of furosemide by GC- or LC-MS. Furosemide is a loop diuretic and an inhibitor of the Na+/K+/2Cl- (NKCC) cotransporters, NKCC1 and NKCC2 (Kis = ~10 µM for both).1,2 In vivo, furosemide (0.1 mg/kg, p.o.) increases diuresis in beagle dogs.3 Furosemide (30 mg/kg) reduces ventricular collagen deposition and fibrosis in a rat model of dilated cardiomyopathy.4 It is also an inhibitor of carbonic anhydrase I (CAI), CAII, and CAIII (Kis = 0.052-0.065 µM) and organic ion transporter 1 (OAT1; Ki = 9.5 µM), as well as a GABAA receptor antagonist.5,6,7
1.Gillen, C.M., Brill, S., Payne, J.A., et al.Molecular cloning and functional expression of the K-Cl cotransporter from rabbit, rat, and human. A new member of the cation-chloride cotransporter familyJ. Biol. Chem.271(27)16237-16244(1996) 2.Markadieu, N., and Delpire, E.Physiology and pathophysiology of SLC12A1/2 transportersPflugers Arch.466(1)91-105(2014) 3.Potter, B.M., Ames, M.K., Hess, A., et al.Comparison between the effects of torsemide and furosemide on the reninangiotensin-aldosterone system of normal dogsJ. Vet. Cardiol.2651-62(2019) 4.Watanabe, K., Sreedhar, R., Thandavarayan, R.A., et al.Comparative effects of torasemide and furosemide on gap junction proteins and cardiac fibrosis in a rat model of dilated cardiomyopathyBiofactors43(2)187-194(2017) 5.Temperini, C., Cecchi, A., Scozzafava, A., et al.Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adductBioorg. Med. Chem. Lett.18(8)2567-2573(2008) 6.Rajan, S.T., Kumar, M.K., and Ramakrishna, M.The novel process for the preparation of (1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]-oxy]acetic acid(2014) 7.Siess, W., Siegel, F.L., and Lapetina, E.G.Dihomogammalinolenic acid, but not eicosapentaenoic acid, activates washed human plateletsBiochim. Biophys. Acta.801(2)265-276(1984)
| Cas No. | 1189482-35-6 | SDF | |
| 别名 | 呋塞米 D5 | ||
| Canonical SMILES | ClC1=C(S(N)(=O)=O)C=C(C(O)=O)C(NC([2H])([2H])C2=C([2H])C([2H])=C([2H])O2)=C1 | ||
| 分子式 | C12H6ClD5N2O5S | 分子量 | 335.8 |
| 溶解度 | DMSO : ≥ 100 mg/mL (297.82 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。 |
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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 | 2.978 mL | 14.8898 mL | 29.7796 mL |
| 5 mM | 0.5956 mL | 2.978 mL | 5.9559 mL |
| 10 mM | 0.2978 mL | 1.489 mL | 2.978 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。
Quantification of furosemide in camel plasma by high resolution mass spectrometry, application on pharmacokinetics
Biomed Chromatogr 2017 Jun;31(6).PMID:27859445DOI:10.1002/bmc.3902.
We developed and validated a high-resolution liquid chromatography mass spectrometry method for the quantification of furosemide in camel plasma which was used for a pharmacokinetic study in camels. Plasma samples were extracted by supported liquid extraction and furosemide and internal standard (Furosemide-d5) were separated on a an Agilent Zorbax XDB C18 column (50 × 2.1 mm i.d., 3.5 μm). Data was acquired in full-scan mode over a mass range of 200-400 Da in negative electrospray mode at a resolution of 70,000. Linear calibration curves were obtained over the concentration ranges of 1.0-10,000 ng/mL. The validated method was then successfully applied in evaluating the pharmacokinetics and metabolites of furosemide in six camels (Camelus dromedarus) and we were able to advice on a withdrawal time of furosemide treatment before racing.
Detection, quantification, and pharmacokinetics of furosemide and its effects on urinary specific gravity following IV administration to horses
Vet Ther 2003 Winter;4(4):350-63.PMID:15136977doi
Furosemide is a potent loop diuretic used for the prevention of exercise-induced pulmonary hemorrhage in horses. This drug may interfere with the detection of other substances by reducing urinary concentrations, so its use is strictly regulated. The regulation of furosemide in many racing jurisdictions is based on paired limits of urinary SG (<1.010) and serum furosemide concentrations (>100 ng/ml). To validate this regulatory mechanism, a liquid chromatography/mass spectrometry/mass spectrometry method employing a solid-phase extraction procedure and Furosemide-d5 as an internal standard was developed. The method was used to determine the pharmacokinetic parameters of furosemide in equine serum samples and its effects on urinary SG after IV administration (250 mg) to 10 horses. Pharmacokinetic analysis showed that serum concentrations of furosemide were well described by a two-compartmental open model. Based on results in this study, it is very unlikely for horses to have serum furosemide concentrations greater than 100 ng/ml or urine SG less than 1.010 at 4 hours after administration (250 mg IV). However, it should be remembered that urine SG is a highly variable measurement in horses, and even without furosemide administration, some horses might naturally have urine SG values less than 1.010.