| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Losartan carboxylic acid (EXP-3174; EXP 3174; EXP3174) is a cytochrome P450-mediated carboxylic acid metabolite, and is an active metabolite of Losartan. Losartan (Cozaar among others) is a recognized antihypertensive medication that blocks the angiotensin II receptor.
| Targets |
binding of [125I]-angiotensin II to VSMC ( IC50 = 1.1 nM )
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|---|---|
| ln Vitro |
Losartan Carboxylic Acid (E-3174) inhibits the specific binding of [125I]-angiotensin II to VSMC with an IC50 of 1.1 nM. In VSMC, the angiotensin II-induced production of inositolphosphates is eliminated by losartan carboxylic acid. With an IC50 of 5 nM, losartan carboxylic acid suppresses the increase in intracellular cytosolic Ca2+ concentration that is brought about by angiotensin II. Losartan Carboxylic Acid is superior to losartan in its ability to inhibit the rise in Egr-1 mRNA brought on by angiotensin II. With an IC50 of 3 nM, losartan carboxylic acid inhibits the angiotensin II-induced cell protein synthesis[1].
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| ln Vivo |
Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) produces a pressor response inhibition (87±4%) comparable to that of angiotensin I[3]. Anesthetized dogs with a recent anterior myocardial infarction (8.1±0.4 days) are given intravenous lossartan carboxylic acid injection. One hour after treatment begins, the left circumflex coronary artery is electrolytically injured to cause posterolateral ischemia and thrombotic occlusion[4].
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| Cell Assay |
For 48 hours, cells were treated with either 15% FBS or Ang II in the presence or absence of the recommended dosage of losartan. Using the MTT assay, cell proliferation was assessed.
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| Animal Protocol |
Mongrel dogs of either sex, weighing 15-25 kg
0.1 mg/kg (followed by 0.02 mg/kg/h) i.v. for 5.5 hours |
| References |
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| Molecular Formula |
C₂₂H₂₁CLN₆O₂
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|---|---|
| Molecular Weight |
436.89
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| Exact Mass |
436.14
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| Elemental Analysis |
C, 60.48; H, 4.85; Cl, 8.11; N, 19.24; O, 7.32
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| CAS # |
124750-92-1
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| Related CAS # |
Losartan-d4 (carboxylic acid); 1246820-62-1; Losartan; 114798-26-4; Losartan potassium; 124750-99-8; Losartan carboxylic acid-d4 hydrochloride
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| Appearance |
Solid powder
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| SMILES |
CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)O)Cl
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| InChi Key |
ZEUXAIYYDDCIRX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21ClN6O2/c1-2-3-8-18-24-20(23)19(22(30)31)29(18)13-14-9-11-15(12-10-14)16-6-4-5-7-17(16)21-25-27-28-26-21/h4-7,9-12H,2-3,8,13H2,1H3,(H,30,31)(H,25,26,27,28)
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| Chemical Name |
2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
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| Synonyms |
Losartan Carboxylic Acid; EXP 3174; EXP-3174; EXP3174; E3174; E-3174; E 3174
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~87 mg/mL (~199.1 mM)
Ethanol: ~87 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2889 mL | 11.4445 mL | 22.8891 mL | |
| 5 mM | 0.4578 mL | 2.2889 mL | 4.5778 mL | |
| 10 mM | 0.2289 mL | 1.1445 mL | 2.2889 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03864042 | Active Recruiting |
Drug: dextromethorphan Drug: losartan |
Advanced Solid Tumors Metastatic Melanoma |
Pfizer | January 2, 2018 | Phase 1 |
| NCT01797926 | Completed | Drug: Reference Treatment: 5 mg amlodipine + 50 mg losartan Drug: Reference Treatment:5 mg amlodipine + 100 mg losartan |
Hypertension | GlaxoSmithKline | May 23, 2013 | Phase 1 |
| NCT01033318 | Completed | Drug: MK1809 Drug: Comparator: Losartan Drug: Comparator: Placebo |
Hypertension | Merck Sharp & Dohme LLC | September 11, 2007 | Phase 1 |
| NCT01713647 | Completed | Drug: Amlodipin, losartan, HCTZ | Fasting | Pharmaceutical Research Unit, Jordan |
October 2012 | Phase 1 |
| NCT01766050 | Completed | Drug: Losartan Drug: Caffeine |
Transplant Rejection | Bristol-Myers Squibb | January 2013 | Phase 4 |
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