Losartan Potassium (DuP 753)
For research use only.
Catalog No.S1359 Synonyms: MK 954
6 publications
CAS No. 124750-99-8
Losartan Potassium (DuP 753, MK 954) is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Selleck's Losartan Potassium (DuP 753) has been cited by 6 publications
3 Customer Reviews
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Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.
Sci Rep, 2015, 5:8116.. Losartan Potassium (DuP 753) purchased from Selleck.
Losartan attenuates the inhibitory effect of METH on SH-SY5Y cell proliferation accompanied with decreased D3R expression. (A) Losartan attenuated the proliferation inhibitory effect of METH on SH-SY5Y cells. n = 3 for each group. Saline, **p < 0.01; 2 mM METH, ##p < 0.01, ###p < 0.001. (B) The DRs and DAT expressions were measured in SH-SY5Y cells with or without losartan treatment. Student’s t test, **p < 0.01, ***p < 0.001, n = 6 for each group. (C) The decreased D3R level was attenuated by losartan in METH-treated SH-SY5Y cells. One-way ANOVA followed by Tukey’s post-tests were performed, **p < 0.01, ***p < 0.001, n = 4 for each group
Neurotherapeutics, 2018, 15(2):500-510. Losartan Potassium (DuP 753) purchased from Selleck.
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Representative Trichrome II Blue staining of heart tissue sections of mice from the sham, TAC, TAC + gallic acid, TAC + losartan, TAC + carvedilol, and TAC + furosemide groups. Blue staining indicates collagen deposition. Scale bar = 100 µm
Sci Rep, 2018, 8(1):9302. Losartan Potassium (DuP 753) purchased from Selleck.
Purity & Quality Control
Choose Selective Angiotensin Receptor Inhibitors
Biological Activity
| Description | Losartan Potassium (DuP 753, MK 954) is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. | ||
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| Features | Losartan has a major active metabolite, EXP 3174. | ||
| Targets |
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| In vivo | Losartan (180 mg/d) causes significant increases in plasma angiotensin II and angiotensin-(1-7) in monkeys with diet-induced hypercholesterolemia. Losartan (180 mg/d) reduces the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% in monkeys with diet-induced hypercholesterolemia. Losartan reduces the susceptibility of LDL to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression in monkeys with diet-induced hypercholesterolemia. [2] Losartan (0.6 g/L in their drinking water) prevents elastic fiber fragmentation and blunted TGF-β signaling in the aortic media in pregnant Fbn1C1039G/+ mice, as evidenced by reduced nuclear accumulation of pSmad2. Losartan (0.6 g/L in their drinking water) shows a reduction in distal airspace caliber in pregnant Fbn1C1039G/+ mice. Losartan (0.6 g/L in their drinking water) improves disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics in pregnant Fbn1C1039G/+ mice. [3] Losartan (5 mg/kg/d) leads to a significant decrease in the development of atherosclerotic lesions in the apo E deficient mice. Losartan (5 mg/kg/d) significantly reduces the susceptibility of the mice LDL to lipid oxidation following its incubation with CuSO4 in the apo E deficient mice. [4] Losartan (10 mg/kg) administration increases blood angiotensin levels four fold to six fold, blood BK levels are unchanged in male Sprague Dawley rats. Losartan (10 mg/kg) increases plasma renin levels 100-fold, plasma angiotensinogen levels decreases to 24% of control and plasma aldosterone levels are unchanged in male Sprague Dawley rats. [5] |
Protocol
| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 92 mg/mL (199.12 mM) |
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| Water | 92 mg/mL (199.12 mM) | |
| Ethanol | 92 mg/mL (199.12 mM) | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing. |
30 mg/mL |
* 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 | 462.01 |
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| Formula | C22H23ClKN6O |
| CAS No. | 124750-99-8 |
| Storage |
powder in solvent |
| Synonyms | MK 954 |
| Smiles | CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4)CO)Cl.[K+] |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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