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Losartan

Catalog No. T0215L CAS 114798-26-4

Synonyms: DuP-753

Losartan (DuP-753) is an angiotensin II receptor antagonist.

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Losartan, CAS 114798-26-4

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Purity: 100%

Purity: 99.79%

Purity: 99.53%

Purity: 99.48%

Purity: 99.37%

Purity: 98.80%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Losartan (DuP-753) is an angiotensin II receptor antagonist.
Targets&IC50	AT1 receptor:20 nM
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 Fbn1C1039 g/+ mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1C1039 g/+ 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 Fbn1C1039 g/+ 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].
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.

Synonyms	DuP-753
Molecular Weight	422.91
Formula	C22H23ClN6O
CAS No.	114798-26-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 198.6 mM

References and Literature

1. Burnier, M. Angiotensin II type 1 receptor blockers. Circulation, 2001. 103(6): p. 904-12. 2. Ashry, O., et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol, 2014. 3. Choi, C.H., et al. Angiotensin II type I receptor and miR-155 in endometrial cancers: synergistic antiproliferative effects of anti-miR-155 and losartan on endometrial cancer cells. Gynecol Oncol, 2012. 126(1): p. 124-31. 4. Habashi, J.P., et al. Losartan, an AT1 antagonist, prevents aortic aneurysm in a mouse model of Marfan syndrome. Science, 2006. 312(5770): p. 117-21. 5. Campbell, D.J., et al. Effects of losartan on angiotensin and bradykinin peptides and angiotensin-converting enzyme. J Cardiovasc Pharmacol, 1995. 26(2): p. 233-40. 6. Zhang L, Zhang B, Yu Y, et al. Angiotensin II Increases HMGB1 Expression in the Myocardium Through AT1 and AT2 Receptors When Under Pressure Overload[J]. International Heart Journal. 2021: 20-384 7. Zhang Y, Song Z, Huang S, et al. Aloe emodin relieves Ang II‐induced endothelial junction dysfunction via promoting ubiquitination mediated NLRP3 inflammasome inactivation[J]. Journal of Leukocyte Biology. 2020, 108(6): 1735-1746.

Citations

1. Zhang Y, Song Z, Huang S, et al. Aloe emodin relieves Ang II‐induced endothelial junction dysfunction via promoting ubiquitination mediated NLRP3 inflammasome inactivation. Journal of Leukocyte Biology. 2020, 108(6): 1735-1746 2. Zhang L, Zhang B, Yu Y, et al. Angiotensin II Increases HMGB1 Expression in the Myocardium Through AT1 and AT2 Receptors When Under Pressure Overload. International Heart Journal. 2021: 20-384

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Drug-induced Liver Injury (DILI) Compound Library Anti-Diabetic Compound Library FDA-Approved Drug Library Anti-Hypertension Compound Library

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Keywords

Losartan 114798-26-4 Endocrinology/Hormones RAAS DuP 753 Angiotensin Receptor DuP753 DuP-753 inhibit Inhibitor inhibitor

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