| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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Purity: ≥98%
Bumetanide (also known as Ro 10-6338; PF-1593) is a novel and potent inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM. Bumetanide is a loop diuretic belonging to the sulfamyl category and is used to treat heart failure, and is often used in people in whom high doses of furosemide are ineffective. Bumetanide is almost completely absorbed (80%), and the absorption is not altered when it is taken with food. It is said to be a more predictable diuretic, meaning that the predictable absorption is reflected in a more predictable effect.
| ln Vitro |
The two main splice forms of human NKCC, hNKCC1A and hNKCC2A, are inhibited by bumetanide [1]. In NKCC1A-expressing oocytes, bumetanide (0.03-100 μM; 5 minutes) suppresses 86Rb+ in a dose-regulated manner [1]. In HEK-293 cells, bumetanide inhibits NKCC2 isoform B with an IC50 value of 0.54 μM[2].
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| ln Vivo |
The administration of bumetanide (7.6-30.4 mg/kg) intravenously prevented a 40–67% reduction in the cutaneous and striatal apparent diffusion coefficient (ADC), a sign of decreased edema development [3]. Additionally, intravenous reductions of bumetanide at doses of 2 mg/kg, 8 mg/kg, and 20 mg/kg are possible [4].
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| Animal Protocol |
Animal/Disease Models: Normotensive SD (SD (Sprague-Dawley)) rats (250-300 g) [3]
Doses: 7.6 mg/kg, 15.2 mg/kg, 30.4 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: diminished middle cerebral artery occlusion (MCAO) ) caused a decrease in ADC values in all four ipsilateral regions (L1-L4). Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (220-300 g) [4] Doses: 2 mg/kg, 8 mg/kg, 20 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)administration Experimental Results: T1/2 (21.4 minutes, 53.8 minutes and 137 minutes for 2 mg/kg, 8 mg/kg and 20 mg/kg respectively) |
| References |
[1]. Lykke K, et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 2016 Jun;59:42-9.
[2]. Ciaran Richardson, et al. Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways. J Cell Sci. 2011 Mar 1;124(Pt 5):789-800. [3]. Martha E O'Donnell, et al. Bumetanide inhibition of the blood-brain barrier Na-K-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J Cereb Blood Flow Metab. 2004 Sep;24(9):1046-56. [4]. S H Lee, et al. Pharmacokinetics and pharmacodynamics of bumetanide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1994 Feb;22(1):1-17.6 |
| Molecular Formula |
C17H20N2O5S
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|---|---|
| Molecular Weight |
364.4161
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| CAS # |
28395-03-1
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| Related CAS # |
Bumetanide-d5;1216739-35-3;Bumetanide sodium;28434-74-4;Bumetanide-d5 Butyl Ester;1216685-32-3
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| SMILES |
O=C(O)C1=CC(S(=O)(N)=O)=C(OC2=CC=CC=C2)C(NCCCC)=C1
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| InChi Key |
MAEIEVLCKWDQJH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N2O5S/c1-2-3-9-19-14-10-12(17(20)21)11-15(25(18,22)23)16(14)24-13-7-5-4-6-8-13/h4-8,10-11,19H,2-3,9H2,1H3,(H,20,21)(H2,18,22,23)
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| Chemical Name |
3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid
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| Synonyms |
PF 1593, PF-1593, PF1593; Ro 10-6338; Ro-10-6338; Ro 10 6338; Trade names: Bumex or Burinex;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~274.41 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7441 mL | 13.7204 mL | 27.4409 mL | |
| 5 mM | 0.5488 mL | 2.7441 mL | 5.4882 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7441 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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