Furosemide sodium
(Synonyms: 呋塞米钠) 目录号 : GC36091
A loop diuretic and an inhibitor of NKCC1 and NKCC2
Cas No.:41733-55-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Furosemide is a loop diuretic and an inhibitor of the Na+/K+/2Cl- (NKCC) cotransporters, NKCC1 and NKCC2 (Kis = ~10 ?M 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 ?M) and organic ion transporter 1 (OAT1; Ki = 9.5 ?M), as well as a GABAA receptor antagonist.5,6,7 This product is also available as an analytical reference standard .
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. Acta801(2)265-276(1984)
| Cas No. | 41733-55-5 | SDF | |
| 别名 | 呋塞米钠 | ||
| Canonical SMILES | O=C([O-])C1=CC(S(=O)(N)=O)=C(Cl)C=C1NCC2=CC=CO2.[Na+] | ||
| 分子式 | C12H10ClN2NaO5S | 分子量 | 352.73 |
| 溶解度 | DMSO: ≥ 150 mg/mL (425.25 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 | 2.835 mL | 14.1751 mL | 28.3503 mL |
| 5 mM | 0.567 mL | 2.835 mL | 5.6701 mL |
| 10 mM | 0.2835 mL | 1.4175 mL | 2.835 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。
Preparation of an amorphous sodium furosemide salt improves solubility and dissolution rate and leads to a faster Tmax after oral dosing to rats
Eur J Pharm Biopharm 2013 Nov;85(3 Pt B):942-51.PMID:24075980DOI:10.1016/j.ejpb.2013.09.002.
Amorphous forms of Furosemide sodium salt and furosemide free acid were prepared by spray drying. For the preparation of the amorphous free acid, methanol was utilised as the solvent, whereas the amorphous sodium salt was formed from a sodium hydroxide-containing aqueous solvent in equimolar amounts of NaOH and furosemide. Information about the structural differences between the two amorphous forms was obtained by Fourier Transform Infrared Spectroscopy (FTIR), and glass transition temperature (Tg) was determined using Differential Scanning Calorimetry (DSC). The stability and devitrification tendency of the two amorphous forms were investigated by X-ray Powder Diffraction (XRPD). The apparent solubility of the two amorphous forms and the crystalline free acid form of furosemide in various gastric and intestinal stimulated media was determined. Moreover, the dissolution characteristics of the two amorphous forms and of crystalline free acid were investigated. FTIR confirmed molecular differences between the amorphous free acid and salt. The amorphous salt showed a Tg of 101.2 °C, whereas the Tg for the amorphous free acid was found to be 61.8 °C. The amorphous free acid was physically stable for 4 days at 22 °C and 33% relative humidity (RH), while the amorphous salt exhibited physical stability for 291 days at the same storage conditions. When storing the amorphous forms at 40 °C and 75% RH both forms converted to crystalline forms after 2 days. The apparent solubility of the amorphous salt form was higher than that of both amorphous and crystalline free acid in all media studied. All three forms of furosemide exhibited a greater solubility in the presence of biorelevant media as compared to buffer, however, an overall trend for a further increase in solubility in relation to an increase in media surfactant concentration was not seen. The amorphous salt demonstrated an 8- and 20-fold higher intrinsic dissolution rate (IDR) when compared to amorphous and crystalline free acid, respectively. The promising properties of the amorphous salt in vitro were further evaluated in an in vivo study, where solid dosage forms of the amorphous salt, amorphous and crystalline free acid and a solution of furosemide were administered orally to rats. The amorphous salt exhibited a significantly faster Tmax compared to the solution and amorphous and crystalline free acid. Cmax for the solution was significantly higher compared to the three furosemide forms. No significant difference was found in AUC and absolute bioavailability for the solution, crystalline free acid and the two amorphous forms of furosemide. It can be concluded that the higher IDR and higher apparent solubility of the amorphous salt resulted in a faster Tmax compared to the amorphous and crystalline free acid.