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Losartan potassium

Cozaar, Lorzaar, Losaprex

An Antagonist of Angiotensin Receptor Type-1

Cat #: L-185
Alternative Name Cozaar, Lorzaar, Losaprex
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 461
    Purity: ≥99%
    Effective concentration 1-100 nM.
    Structure
    Chemical name potassium;[2-butyl-5-chloro-3-[[4-[2-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol.
    Molecular formula C22H22ClKN6O.
    CAS No.: 124750-99-8
    PubChem CID 11751549
    Activity Losartan potassium is an Angiotensin II Type 1 receptor antagonist1.
    References-Activity
    1. Ji, H. et al. (1994) J. Biol. Chem. 269, 16533.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 200 mM in H2O or DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Losartan potassium inhibits the activation of AT1R expressed in CHO-K1-mt aequorin-Gα16 cells.
      Alomone Labs Losartan potassium inhibits the activation of AT1R expressed in CHO-K1-mt aequorin-Gα16 cells.
      Dose-response curve for the inhibition of AT1R expressed in CHO-K1-mt aequorin-Gα16 cells. Ca2+ response, as detected by elevation in aequorin derived fluorescence following 0.04 nM Angiotensin II application, was inhibited by increasing concentrations of Losartan potassium (#L-185). 20 nM Losartan potassium fully inhibited the activation by Angiotensin II.
    References - Scientific background
    1. Kurtz, T.W. et al. (2012) Vasc. Health Risk Manag. 8, 133.
    2. Han, X. et al. (2015) Eur. J. Med. Chem. 103, 473.
    3. Tchekalarova, J.D. et al. (2015) Cell. Mol. Neurobiol. 36, 927.
    Scientific background

    Angiotensin II is responsible for vasoconstriction in the renin-angiotensin system. In addition to its direct effect on blood vessels it stimulates the synthesis and release of aldosterone and also promotes renal tubular reabsorption of sodium, resulting in water retention1.

    Losartan potassium (Cozaar, Loszaar, Losaprex) is a synthetic antagonist of the Angiotensin II type 1 receptor with an effective concentration of 1-100 nM and an IC50 of 5 nM2. Losartan is used for the treatment of hypertension and heart failure, especially with patients who suffer from severe cough due to ACE inhibitor intake. It also improves the prognosis of diabetic nephropathy and reduces the risk of CVA in patients with left ventricle hypertrophy. Maximum effect is reached 3-6 weeks after beginning of treatment. Interestingly, long term treatment with Losartan in a model of hypertensive and epileptic mice yielded neuroprotective results. These mice are characterized by elevated activity of the renin-angiotensin system and a higher level of Angiotensin receptors than other mouse models. Losartan delayed the onset of epileptic seizures and reduced their amount and duration. Neuroprotection was mostly demonstrated in the CA3 area of the hippocampus and the septo-temporal hilus of the dentate gyrus3.

    Target AT1R receptors
    Lyophilized Powder
    Last update: 25/04/2021

    Losartan potassium (#L-185) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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