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[CAS NO. 27589-33-9] Azosemide
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-107321 |
| Brand: | MCE |
| CAS: | 27589-33-9 |
Overview
| MDL | MFCD00867321 |
|---|---|
| Molecular Weight | 370.84 |
| Molecular Formula | C12H11ClN6O2S2 |
| SMILES | ClC1=CC(NCC2=CC=CS2)=C(C3=NN=NN3)C=C1S(N)(=O)=O |
2 Publications Citing Use of MCE
Summary
Azosemide, a sulfonamide loop diuretic, is a potent NKCC1 inhibitor with IC 50 s of 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B, respectively [1] .
IC50 & Target
IC50: 0.246 µM (hNKCC1A) and 0.197 µM (NKCC1B) [1]
In Vitro
Azosemide inhibits the sodium-potassium-chloride-cotransporter human variants hNKCC1A and hNKCC1B [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley rats (control rats, weighing 310345 g) and NARs (weighing 220315 g) of 9 weeks of age [2] |
| Dosage: | 10 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Infused over 1 min via the jugular vein (i.v.) |
| Result: | Showed 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00355667 | Hyogo College of Medicine|Ministry of Health, Labour and Welfare, Japan |
Congestive Heart Failure
|
June 2006 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 674.15 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6966 mL | 13.4829 mL | 26.9658 mL |
| 5 mM | 0.5393 mL | 2.6966 mL | 5.3932 mL |
| 10 mM | 0.2697 mL | 1.3483 mL | 2.6966 mL |
References
- [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.
Synonyms
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