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Azosemide

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Chemical Structure| 27589-33-9 同义名 : -
CAS号 : 27589-33-9
货号 : A171703
分子式 : C12H11ClN6O2S2
纯度 : 97%
分子量 : 370.838
MDL号 : MFCD30541344
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(674.15 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Azosemide, a sulfonamide loop diuretic, was the most potent NKCC1 inhibitor (IC50s 0.246 µM for hNKCC1A and 0.197 µM for NKCC1B), being about 4-times more potent than bumetanide. Azosemide inhibits the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B[3]. After oral administration of the same dose of azosemide and furosemide, the diuretic effect was similar between the two drugs, but after intravenous administration, the effect of azosemide was 5.5-8 times greater than that in furosemide[4]. Azosemide was absorbed from all regions of GI tract studied and approximately 93.5, 79.1, 86.1, and 71.5% of the doses (5, 10, 20, and 30 mg/kg, respectively) were absorbed between 1 and 24 hr after oral administration[5]. Azosemide is a new monosulfamyl diuretic which inhibits solute transport throughout the thick ascending limb of the loop of Henle. Azosemide 40 mg caused less potassium excretion than 40 mg of furosemide but there was no significant difference in the sodium/potassium excretion ratio[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.48mL

2.70mL

1.35mL

26.97mL

5.39mL

2.70mL

参考文献

[1]Hampel P, et al. Azosemide is more potent than bumetanide and various other loop diuretics to inhibit the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B. Sci Rep. 2018 Jun 29;8(1):9877.

[2]Kim EJ, et al. Pharmacokinetics and pharmacodynamics of intravenous azosemide in mutant Nagaseanalbuminemic rats. Drug Metab Dispos. 2003 Feb;31(2):194-201.

[3]Hampel P, Römermann K, MacAulay N, Löscher W. Azosemide is more potent than bumetanide and various other loop diuretics to inhibit the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B. Sci Rep. 2018 Jun 29;8(1):9877

[4]Suh OK, Kim SH, Lee MG. Pharmacokinetics and pharmacodynamics of azosemide. Biopharm Drug Dispos. 2003 Oct;24(7):275-97

[5]Lee SH, Lee MG. Pharmacokinetics and pharmacodynamics of azosemide after intravenous and oral administration to rats: absorption from various GI segments. J Pharmacokinet Biopharm. 1996 Dec;24(6):551-68

[6]Brater DC, Anderson SA, Strowig S. Azosemide, a "loop" diuretic, and furosemide. Clin Pharmacol Ther. 1979 Apr;25(4):435-9