Losartan
Catalog No.S5067
Molecular Weight(MW): 422.91
Losartan 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.
Cited by 1 publication
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Biological Activity
| Description | Losartan 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. | ||
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| 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]. |
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| 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]. |
Protocol
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Solubility (25°C)
| In vitro | DMSO | 84 mg/mL (198.62 mM) |
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* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 422.91 |
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| Formula | C22H23ClN6O |
| CAS No. | 114798-26-4 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03435939 | Not yet recruiting | Cystic Fibrosis | University of Kansas Medical Center | March 10 2019 | Early Phase 1 |
| NCT03435939 | Not yet recruiting | Cystic Fibrosis | University of Kansas Medical Center | March 10 2019 | Early Phase 1 |
| NCT03692013 | Not yet recruiting | HypertensionNephropathy | Fifth Affiliated Hospital Sun Yat-Sen University|Third Affiliated Hospital Sun Yat-Sen University | December 1 2018 | Phase 4 |
| NCT03692013 | Not yet recruiting | HypertensionNephropathy | Fifth Affiliated Hospital Sun Yat-Sen University|Third Affiliated Hospital Sun Yat-Sen University | December 1 2018 | Phase 4 |
| NCT03632213 | Recruiting | Mucopolysaccharidosis IV A|Mucopolysaccharidosis VI|Mucopolysaccharidoses|MPS IV A|MPS VI|MPS - Mucopolysaccharidosis|Morquio A Syndrome|Morquio Syndrome A|Morquio Syndrome | Hospital de Clinicas de Porto Alegre|The Isaac Foundation | November 7 2018 | Phase 2 |
| NCT03603938 | Not yet recruiting | Chronic Kidney Disease Patients | Fifth Affiliated Hospital Sun Yat-Sen University | November 1 2018 | Not Applicable |
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