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 No. 114798-26-4

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Losartan Related Products

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
NCT06329050 Recruiting
Healthy
University of Electronic Science and Technology of China
 March 5 2024 Not Applicable
NCT06329076 Recruiting
Healthy
University of Electronic Science and Technology of China
 March 5 2024 Not Applicable
NCT05402397 Recruiting
Uric Acid Nephropathy
Hospital General de Niños Pedro de Elizalde
 July 1 2022 Phase 4
NCT05407220 Unknown status
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

Chemical Information & 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

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


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