| Bioactivity | Azosemide, a sulfonamide loop diuretic, is a potent NKCC1 inhibitor with IC50s of 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B, respectively[1]. | ||||||||||||
| Target | IC50: 0.246 µM (hNKCC1A) and 0.197 µM (NKCC1B) | ||||||||||||
| Invitro | Azosemide inhibits the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B[1]. | ||||||||||||
| In Vivo | Azosemide shows a smaller AUC (81.9% decrease), shorter terminal half-life (50.9% decrease) and MRT (64.1% decrease), faster CL (454% increase), CLR (853% increase) and CLNR (307% increase) for NARs[2]. Animal Model: | ||||||||||||
| Name | Azosemide | ||||||||||||
| CAS | 27589-33-9 | ||||||||||||
| Formula | C12H11ClN6O2S2 | ||||||||||||
| Molar Mass | 370.84 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |