[CAS NO. 27589-33-9] Azosemide

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PRODUCTS SPECIFICATIONS [27589-33-9]

Catalog

HY-107321

Brand

MCE

CAS

27589-33-9

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : 250 mg/mL ( 674.15 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.17 mg/mL (5.85 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.17 mg/mL (5.85 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Benzenesulfonamide, 2-chloro-5-(2H-tetrazol-5-yl)-4-[(2-thienylmethyl)amino]-

Sulfanilamide, 2-chloro-5-(1H-tetrazol-5-yl)-N⁴-2-thenyl-

Benzenesulfonamide, 2-chloro-5-(1H-tetrazol-5-yl)-4-[(2-thienylmethyl)amino]-

2-Chloro-5-(2H-tetrazol-5-yl)-4-[(2-thienylmethyl)amino]benzenesulfonamide

5-(4-Chloro-5-sulfamoyl-2-thenylaminophenyl)tetrazole

Ple 1053

Azosemide

2-Chloro-5-(1H-tetrazol-5-yl)-4-[(2-thienylmethyl)amino]benzenesulfonamide

SK 110 (pharmaceutical)

SK 110

Luret

Diart

Diurapid

2-Chloro-5-(2H-tetrazol-5-yl)-4-(thiophen-2-ylmethylamino)benzenesulfonamide