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阿佐塞米 /Azosemide {[allProObj[0].p_purity_real_show]}

货号:A171703

Azosemide是一种磺胺类袢利尿剂,是 NKCC1 的强效抑制剂,IC50 值分别为 0.246 μM 和 0.197 μM。

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Azosemide 化学结构 CAS号:27589-33-9
Azosemide 化学结构
CAS号:27589-33-9
Azosemide 3D分子结构
CAS号:27589-33-9
Azosemide 化学结构 CAS号:27589-33-9
Azosemide 3D分子结构 CAS号:27589-33-9
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Azosemide 纯度/质量文件 产品仅供科研

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Azosemide 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].

Azosemide 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

Azosemide 实验方案

计算器
存储液制备 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

Azosemide 技术信息

CAS号27589-33-9
分子式C12H11ClN6O2S2
分子量 370.838
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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