Losartan

SKU: orb1310825

Description

Losartan, also known as DuP-753, is a selective antagonist of the angiotensin II type 1 (AT1) receptor. It is widely used in research to study the renin-angiotensin system in models of hypertension, cardiovascular disease, and renal function, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 114798-26-4
• MW: 422.91
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₂₃ClN₆O
• SMILES: CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1
• Target: RAAS
• Solubility: DMSO:125 mg/mL (295.57 mM);Saline:33.3 mg/mL (78.74 mM)

Bioactivity

• Target IC50:
  AT1 receptor:20 nM
• In Vivo:
  Losartan (0.6 g/L, p.o.)-treated Fbn1C1039 g/+ mice show reduced distal airspace caliber compared to placebo-treated counterparts. The dosages of losartan and propranolol are titrated to achieve similar hemodynamic effects. Analysis of pSmad2 nuclear staining indicates that losartan antagonizes TGF-β signaling in the aortic wall of Fbn1C1039 g/+ mice, improving lung disease manifestations independently of hemodynamics. Losartan (10 mg/kg, intraarterial injection) increases blood angiotensin levels by four- to sixfold. Losartan (10 mg/kg, i.p.) increases plasma renin levels by 100-fold, decreases plasma angiotensinogen levels to 24% of control, and leaves plasma aldosterone levels unchanged.
• In Vitro:
  Losartan competes with the binding of angiotensin II to AT1 receptors, with an IC50 of 20 nM. At 40 μM, losartan affects ISC and prevents the effect of ANGII on ISC. It significantly reduces Ang II-mediated cell proliferation in endometrial cancer cells, with a greater antiproliferative effect when combined with anti-miR-155 compared to each drug alone.
• Cell Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Angiotensin Receptor, AT1 receptor, DuP 753, DuP753, DuP-753, inhibit, Losartan, Inhibitor

Compound Identifiers

PubChem CID

3961