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Losartan Potassium (DuP 753)

Name: Losartan Potassium (DuP 753)
Brand: Selleck Chemicals
SKU: S1359
Rating: 5 (9 reviews)

Catalog No.S1359 Synonyms: MK 954

For research use only.

Losartan Potassium (DuP 753, MK 954) is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

Losartan Potassium (DuP 753) Chemical Structure

CAS No. 124750-99-8

Selleck's Losartan Potassium (DuP 753) has been cited by 9 Publications

3 Customer Reviews

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Biological Activity

Description

Losartan Potassium (DuP 753, MK 954) is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

Features

Losartan has a major active metabolite, EXP 3174.

Targets

AT1 receptor ^[1]

20 nM

In vivo

Losartan (180 mg/d) causes significant increases in plasma angiotensin II and angiotensin-(1-7) in monkeys with diet-induced hypercholesterolemia. Losartan (180 mg/d) reduces the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% in monkeys with diet-induced hypercholesterolemia. Losartan reduces the susceptibility of LDL to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression in monkeys with diet-induced hypercholesterolemia. ^[2] Losartan (0.6 g/L in their drinking water) prevents elastic fiber fragmentation and blunted TGF-β signaling in the aortic media in pregnant Fbn1^C1039G/+ mice, as evidenced by reduced nuclear accumulation of pSmad2. Losartan (0.6 g/L in their drinking water) shows a reduction in distal airspace caliber in pregnant Fbn1^C1039G/+ mice. Losartan (0.6 g/L in their drinking water) improves disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics in pregnant Fbn1^C1039G/+ mice. ^[3] Losartan (5 mg/kg/d) leads to a significant decrease in the development of atherosclerotic lesions in the apo E deficient mice. Losartan (5 mg/kg/d) significantly reduces the susceptibility of the mice LDL to lipid oxidation following its incubation with CuSO4 in the apo E deficient mice. ^[4] Losartan (10 mg/kg) administration increases blood angiotensin levels four fold to six fold, blood BK levels are unchanged in male Sprague Dawley rats. Losartan (10 mg/kg) increases plasma renin levels 100-fold, plasma angiotensinogen levels decreases to 24% of control and plasma aldosterone levels are unchanged in male Sprague Dawley rats. ^[5]

Protocol (from reference)

Animal Research:^[2]	Animal Models: Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ Dosages: 180 mg/d Administration: Dietary (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	92 mg/mL (199.12 mM)
	Water	92 mg/mL (199.12 mM)
	Ethanol	92 mg/mL (199.12 mM)
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing.	30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	462.01
Formula	C₂₂H₂₃ClKN₆O
CAS No.	124750-99-8
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4)CO)Cl.[K+]

Download Losartan Potassium (DuP 753) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00880386	Withdrawn	Drug: Losartan	Dyspnea\|Lung Cancer\|Pulmonary Complications\|Radiation Fibrosis	University of South Florida\|National Cancer Institute (NCI)	March 2009	Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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