1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Losartan

Losartan (Synonyms: DuP-753)

Cat. No.: HY-17512 Purity: 99.24%
Handling Instructions

Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

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

Losartan Chemical Structure

Losartan Chemical Structure

CAS No. : 114798-26-4

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
5 g USD 132 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Losartan:

Top Publications Citing Use of Products

    Losartan purchased from MCE. Usage Cited in: FASEB J. 2018 Sep;32(9):5051-5062.

    HUVECs are starved for 12 h, treated with 10 mg/mL (9.56 μM) of AngII with or without Losartan or PD123319 for 12 h, and are subsequently used for Western blot analysis.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

    IC50 & Target

    IC50: 20 nM (angiotensin II)

    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 nM[1]. Losartan (40 μM) affects ISC but prevents the effect of ANGII on ISC[2]. Losartan significantly reduces Ang II-mediated cell proliferation in endometrial cancer cells. The combination of losartan and anti-miR-155 has a significantly greater antiproliferative effect compared to each drug alone[3].

    In Vivo

    Losartan (0.6 g/L, p.o.) -treated Fbn1C1039G/+ mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1C1039G/+ animals. The doses of losartan and propranolol are titrated to achieve comparable hemodynamic effects. Analysis of pSmad2 nuclear staining reveals that losartan antagonizes TGF-β signaling in the aortic wall of Fbn1C1039G/+ mice. Losartan can improve disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics[4]. Losartan (10 mg/kg, intraarterial injection) increases blood angiotensin levels four- to sixfold. Losartan (10 mg/kg, i.p.) increases plasma renin levels 100-fold; plasma angiotensinogen levels decreases to 24% of control; and plasma aldosterone levels are unchanged[5].

    Clinical Trial
    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 : ≥ 100 mg/mL (236.46 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3646 mL 11.8228 mL 23.6457 mL
    5 mM 0.4729 mL 2.3646 mL 4.7291 mL
    10 mM 0.2365 mL 1.1823 mL 2.3646 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [3]

    An MTT assay is used to measure cell proliferation and viability. For the assay, 5000 cells in 200 μL media per well are seeded in a 96 well plate. After overnight incubation to allow for cell attachment, the medium is removed by suction. MTT at 1 mg/mL concentration in serum-free medium is added and then incubated for 4 h at 37°C. After removal of MTT solution, 100 μL of DMSO is added to dissolve formazan crystals. Absorbance at 570 nm and at 600 nm as a reference is then measured using a microplate reader. The difference in absorbance is thus relative to the extent of cell survival.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Female Fbn1C1039G/+ mice undergo timed matings with wild-type male mice. At 14.5d post-coitum, pregnant female Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=10), propranolol (0.5 g/L; n=6) or placebo (n=12). Therapy is continued throughout lactation and after weaning until 10 months of age. Mice are sacrificed and examined using the techniques described above. Propranolol is used for comparison with losartan because β-adrenergic receptor blockade is the current albeit controversial standard of care to modulate abnormal growth of the aortic root in MFS. Beginning at 7 weeks of age, wild-type and Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=5), propranolol (0.5 g/L; n=7) or placebo (n=10). Mice are continued on oral therapy for 6 months and then sacrificed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    422.91

    Formula

    C₂₂H₂₃ClN₆O

    CAS No.

    114798-26-4

    SMILES

    OCC1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Cat. No.:
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    Cat. No.: HY-17512