Home GPCR & G Protein Angiotensin Receptor antagonist Losartan For research use only.

Losartan

Synonyms: DuP-753

Losartan(DuP-753) is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement.

Losartan Chemical Structure

Losartan Chemical Structure

CAS: 114798-26-4

Selleck's Losartan has been cited by 19 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Losartan(DuP-753) is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement.
Targets
AT1 receptor [1]
20 nM
In vitro
In vitro

In vitro, losartan competes with the binding of angiotensin II to AT1 receptors; the concentration that inhibits 50% of the binding of angiotensin II (IC50) is 20 nmol/L[1]. Losartan increases AMPK phosphorylation in a time- and dose-dependent manner in VSMCs. It also increases ACC phosphorylation, a major downstream target protein in the AMPK signaling cascade, and LKB1 phosphorylation, which is an upstream kinase of AMPK. Losartan increases p53 and p21 expression in a time-dependent manner, whereas the levels of p27 are not changed. Losartan suppresses Ang II-induced Rb phosphorylation, as well as cyclin D and cyclin E expression which are required for cell cycle progression. The mechanism of growth suppression by losartan is therefore G0/G1 cell cycle arrest which is reversed by AMPK inhibition, such as compound C or AMPK siRNA, but not by apoptosis[2].
Cell Research Cell lines VSMCs
Concentrations 0, 1, 5, 10 μM
Incubation Time 48 h
Method

Cells were treated with Ang II or 15% FBS in the presence or absence of indicated concentration of losartan for 48 hrs. Cell proliferation was determined by the MTT assay.
In Vivo
In vivo

Losartan has a major active metabolite, EXP 3174. Administered intravenously, EXP3174 is 10 to 20 times more potent than losartan and has a longer duration of action than losartan. However, the oral bioavailability of EXP 3174 is very low. Losartan has a bioavailability of about 33%, the half-life averages 2 h (6-9 hours), and the rate of protein binding is 98.7% when dosed at 50-100 mg/d[1]. Treatment with losartan ameliorates the loss in the number and function of endothelial progenitor cells (EPCs) in hypertensive rats[3].
Animal Research Animal Models 12-week-old male Wistar-Kyoto (WKY) rats and SHR-SP
Dosages 10 mg/kg/day
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05402397 Recruiting Uric Acid Nephropathy Hospital General de Niños Pedro de Elizalde July 1 2022 Phase 4
NCT05407220 Not yet recruiting Healthy Hanmi Pharmaceutical Company Limited June 8 2022 Phase 1
NCT05012631 Recruiting Sickle Cell Disease|Diffuse Myocardial Fibrosis Children''s Hospital Medical Center Cincinnati September 1 2021 Phase 2
NCT05191563 Completed Healthy Hanmi Pharmaceutical Company Limited July 31 2021 Phase 1
NCT04842981 Terminated Arthritis Rheumatoid|Interaction University of Southern Denmark|Odense University Hospital|Hospital of South West Jutland|King Christian X´Hospital for Rheumatic Diseases|Sygehus Lillebaelt|Odense Patient Data Explorative Network May 25 2021 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 422.91 Formula

C22H23ClN6O
CAS No. 114798-26-4 SDF --
Smiles CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CO)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (198.62 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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