Losartan (potassium) [124750-99-8]
Cat# HY-17512A-5g
Size : 5g
Brand : MedChemExpress
Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
For research use only. We do not sell to patients.
Losartan potassium Chemical Structure
CAS No. : 124750-99-8
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This product is a controlled substance and not for sale in your territory.
- HUVECs are starved for 12 h, treated with 10 mg/mL (9.56 μM) of AngII with or without Losartan or PD123319 for 12 h, and are subsequently used for Western blot analysis.
Biological Activity
Protocol
Purity & Documentation
References
Customer Review
Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM. | ||||||||||||||||
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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. Losartan (40 μM) affects ISC but prevents the effect of ANGII on ISC. 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. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
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In Vivo | Losartan (0.6 g/L, p.o.) -treated Fbn1C1039G/+ mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1C1039G/+ 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 Fbn1C1039G/+ mice. Losartan can improve disease manifestations in the lungs, an event that cannot plausibly relate to improved hemodynamics. 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. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||||||||
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461.00 | ||||||||||||||||
C22H22ClKN6O | ||||||||||||||||
124750-99-8 | ||||||||||||||||
Solid | ||||||||||||||||
White to off-white | ||||||||||||||||
OCC1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=N[N-]N=N4)C=C2.[K+] | ||||||||||||||||
Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
4°C, sealed storage, away from moisture *In solvent : -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture) | ||||||||||||||||
In Vitro: DMSO : ≥ 110 mg/mL (238.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : 50 mg/mL (108.46 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. Preparing Stock Solutions
View the Complete Stock Solution Preparation Table * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo: For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments. Calculation results: Working solution concentration: mg/mL This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details. The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE). | ||||||||||||||||
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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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Female Fbn1C1039G/+ mice undergo timed matings with wild-type male mice. At 14.5d post-coitum, pregnant female Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=10), propranolol (0.5 g/L; n=6) or placebo (n=12). Therapy is continued throughout lactation and after weaning until 10 months of age. Mice are sacrificed and examined using the techniques described above. Propranolol is used for comparison with losartan because β-adrenergic receptor blockade is the current albeit controversial standard of care to modulate abnormal growth of the aortic root in MFS. Beginning at 7 weeks of age, wild-type and Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=5), propranolol (0.5 g/L; n=7) or placebo (n=10). Mice are continued on oral therapy for 6 months and then sacrificed. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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[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.
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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H2O / DMSO | 1 mM | 2.1692 mL | 10.8460 mL | 21.6920 mL | 54.2299 mL |
5 mM | 0.4338 mL | 2.1692 mL | 4.3384 mL | 10.8460 mL | |
10 mM | 0.2169 mL | 1.0846 mL | 2.1692 mL | 5.4230 mL | |
15 mM | 0.1446 mL | 0.7231 mL | 1.4461 mL | 3.6153 mL | |
20 mM | 0.1085 mL | 0.5423 mL | 1.0846 mL | 2.7115 mL | |
25 mM | 0.0868 mL | 0.4338 mL | 0.8677 mL | 2.1692 mL | |
30 mM | 0.0723 mL | 0.3615 mL | 0.7231 mL | 1.8077 mL | |
40 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 mL | |
50 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0846 mL | |
60 mM | 0.0362 mL | 0.1808 mL | 0.3615 mL | 0.9038 mL | |
80 mM | 0.0271 mL | 0.1356 mL | 0.2711 mL | 0.6779 mL | |
100 mM | 0.0217 mL | 0.1085 mL | 0.2169 mL | 0.5423 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
- GPCR/G Protein
- Angiotensin Receptor
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Losartan124750-99-8DuP-753DuP753DuP 753Angiotensin ReceptorInhibitorinhibitorinhibit
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