Losartan [114798-26-4]
Cat# HY-17512-5g
Size : 5g
Brand : MedChemExpress
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Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
For research use only. We do not sell to patients.
Losartan Chemical Structure
CAS No. : 114798-26-4
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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 is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with 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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| 422.91 | ||||||||||||||||
| C22H23ClN6O | ||||||||||||||||
| 114798-26-4 | ||||||||||||||||
| Solid | ||||||||||||||||
| White to light yellow | ||||||||||||||||
| OCC1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2 | ||||||||||||||||
Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
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| In Vitro: DMSO : ≥ 100 mg/mL (236.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" 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.
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: Select the appropriate dissolution method based on your experimental animal and administration route. For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
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. Please enter your animal formula composition: % DMSO + % + % Tween-80 + % Saline The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE). Calculation results: Working solution concentration: mg/mL Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL). 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). Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline. If the continuous dosing period exceeds half a month, please choose this protocol carefully. Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution. | ||||||||||||||||
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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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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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| DMSO | 1 mM | 2.3646 mL | 11.8228 mL | 23.6457 mL | 59.1142 mL |
| 5 mM | 0.4729 mL | 2.3646 mL | 4.7291 mL | 11.8228 mL | |
| 10 mM | 0.2365 mL | 1.1823 mL | 2.3646 mL | 5.9114 mL | |
| 15 mM | 0.1576 mL | 0.7882 mL | 1.5764 mL | 3.9409 mL | |
| 20 mM | 0.1182 mL | 0.5911 mL | 1.1823 mL | 2.9557 mL | |
| 25 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3646 mL | |
| 30 mM | 0.0788 mL | 0.3941 mL | 0.7882 mL | 1.9705 mL | |
| 40 mM | 0.0591 mL | 0.2956 mL | 0.5911 mL | 1.4779 mL | |
| 50 mM | 0.0473 mL | 0.2365 mL | 0.4729 mL | 1.1823 mL | |
| 60 mM | 0.0394 mL | 0.1970 mL | 0.3941 mL | 0.9852 mL | |
| 80 mM | 0.0296 mL | 0.1478 mL | 0.2956 mL | 0.7389 mL | |
| 100 mM | 0.0236 mL | 0.1182 mL | 0.2365 mL | 0.5911 mL |
- GPCR/G Protein
- Angiotensin Receptor
- Do most proteins show cross-species activity?
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:
Losartan114798-26-4DuP-753DuP753DuP 753Angiotensin ReceptorInhibitorinhibitorinhibit
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