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Submit ReviewLosartan potassium
Description: Selective, non-peptide AT1 antagonist
Alternative Names: DuP-753
Chemical Name: 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol potassium salt
Purity: ≥99% (HPLC)
Biological Activity
Selective non-peptide angiotensin AT1 receptor antagonist. Inhibits the contractile effects of angiotensin II on rabbit aorta and jugular vein (pA2 = 8.27). Orally active antihypertensive agent. Attenuates lung damage in a mouse model of SARS-CoV infection.
Compound Libraries
Losartan potassium is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 461 |
| Formula | C22H22ClKN6O |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 124750-99-8 |
| PubChem ID | 11476710 |
| InChI Key | OXCMYAYHXIHQOA-UHFFFAOYSA-N |
| Smiles | CCCCC1=NC(Cl)=C(CO)N1CC2=CC=C(C3=CC=CC=C3C(N=N4)=NN4[K])C=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 46.1 | 100 | |
| DMSO | 46.1 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 461. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.17 mL | 10.85 mL | 21.69 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Wong et al (1990) Functional studies of nonpeptide angiotensin II receptor subtype-specific ligands: DuP 753 (AII-1) and PD123177 (AII-2). J.Pharmacol.Exp.Ther. 255 584 PMID: 2243344
Wong et al (1990) Nonpeptide angiotensin II receptor antagonists. VIII. Characterization of functional antagonism displayed by DuP an orally active antihypertensive agent. J.Pharmacol.Exp.Ther. 252 719 PMID: 2179531
Rhaleb et al (1991) DuP 753 is a specific antagonist for the angiotensin receptor. Hypertension 17 480 PMID: 1672862
Kuba et al (2005) A crucial role of angiotensin converting enzyme 2 (ACE2) in SARS coronavirus-induced lung injury. Nat.Med. 11 875 PMID: 16007097
If you know of a relevant reference for Losartan potassium, please let us know.
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8 Citations for Losartan potassium
Citations are publications that use Tocris products. Selected citations for Losartan potassium include:
Lee et al (2019) Extracorporeal shock waves protect cardiomyocytes from DOX-induced cardiomyopathy by upregulating survivin via the integrin-ILK-Akt-Sp1/p53 axis. Sci Rep 9 12149 PMID: 31434946
Santhekadur et al (2014) Staphylococcal nuclease domain containing-1 (SND1) promotes migration and invasion via angiotensin II type 1 receptor (AT1R) and TGFβ signaling. FEBS Open Bio 4 353 PMID: 24918049
Leite-Moreira et al (2006) Angiotensin II acutely decreases myocardial stiffness: a novel AT1, PKC and Na+/H+ exchanger-mediated effect. Br J Pharmacol 147 690 PMID: 16415904
Thieme and Oliveira-Souza (2015) Renal hemodynamic and morphological changes after 7 and 28 days of leptin treatment: the participation of angiotensin II via the AT1 receptor. PLoS One 10 e0122265 PMID: 25793389
Fang et al (2013) Compromised regulation of tissue perfusion and arteriogenesis limit, in an AT1R-independent fashion, recovery of ischemic tissue in Cx40(-/-) mice. Am J Physiol Heart Circ Physiol 304 H816 PMID: 23292716
Dominska et al (2018) Angiotensin 1-7 modulates molecular and cellular processes central to the pathogenesis of prostate cancer. Sci.Rep. 8 15772 PMID: 30361641
Tsai et al (2012) Brain-derived neurotrophic factor ameliorates brain stem cardiovascular dysregulation during experimental temporal lobe status epilepticus. EMBO Mol Med 7 e33527 PMID: 22442695
Bhattachariya et al (2014) PYK2 selectively mediates signals for growth versus differentiation in response to stretch of spontaneously active vascular smooth muscle. Physiol Rep 2 PMID: 25347863
Do you know of a great paper that uses Losartan potassium from Tocris? Please let us know.
Reviews for Losartan potassium
Average Rating: 5 (Based on 1 Review.)
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Losartan as type 1 angiotensin II receptor antagonist in piglet study.
By
Hiteshkumar Soni on 01/10/2018
Assay Type: In Vivo
Species: Other
We used Losartan as type 1 angiotensin II receptor antagonist in piglet study to prove that hUII-induced MAP elevation and hemodynamic changeswere inhibited by urantide, a UTR antagonist, but not with losartan.
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