Losartan Carboxylic Acid (Synonyms: E-3174,EXP-3174) |
| رقم الكتالوجGC12512 |
حمض اللوزارتان الكربوكسيل (E-3174) ، مستقلب حمض الكربوكسيل النشط من اللوسارتان ، هو مضاد لمستقبلات الأنجيوتنسين 2 من النوع 1 (AT1)
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Cas No.: 124750-92-1
Sample solution is provided at 25 µL, 10mM.
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Ki = 5-20 nM
Losartan Carboxylic Acid, also named E-3174, a physiologically active metabolite of losartan, is a non-peptide, potent angiotensin II (AII) receptor, type 1 (AT1) antagonist, which inhibits the AII induced cellular responses. AII is the primary mediator of the reninangiotensin system, which regulates the blood pressure and body-fluid balance and may be associated with the development of cardiovascular diseases via increasing contractility and cell growth in vascular smooth muscle cells (VSMC).
In vitro: E-3174 potently blocked the specific binding of [125I]-AII to VSMC isolated from rat aorta. E-3174 was able to dampen the platelet-derived growth factor-induced increase in cell DNA synthesis and protein, which led to the blockade of the AII-induced increase in cell protein [1].
In vivo: Rats were administrated E-3174 intravenously at a dose of l.0 mg/kg. After 6 hours, E-3174 markedly attenuated the cardiovascular effects of AII in rats. E-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2].
References:
[1]. Li, X. & Widdop, R. Angiotensin Type I Receptor Antagonists CY-11974 and EXP 3174 Cause Selective Renal Vasodilatation in Conscious Spontaneously Hypertensive Rats. Clinical Science, 1996; 91(2): 147-154.
[2]. Sachinidis, A., Ko, Y., Weisser, P., zu BricBkwedde, M., Dsing, R., & Christian, R. et al. EXP3174, a metabolite of losartan (MK954, DuP753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. Journal of Hypertension. 1993; 11(2): 155-162.
| Cas No. | 124750-92-1 | SDF | |
| المرادفات | E-3174,EXP-3174 | ||
| Chemical Name | 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid | ||
| Canonical SMILES | [H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(CN4C(C(O)=O)=C(Cl)N=C4CCCC)C=C3 | ||
| Formula | C22H21ClN6O2 | M.Wt | 436.9 |
| الذوبان | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2889 mL | 11.4443 mL | 22.8885 mL |
| 5 mM | 0.4578 mL | 2.2889 mL | 4.5777 mL |
| 10 mM | 0.2289 mL | 1.1444 mL | 2.2889 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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