| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
AT1 Receptor
Losartan D4 targets the angiotensin II type 1 (AT₁) receptor, which is a G protein-coupled receptor involved in the renin-angiotensin system. By blocking AT₁ receptors, losartan prevents angiotensin II-mediated vasoconstriction, aldosterone release, and sympathetic activation. This leads to vasodilation, reduced blood pressure, and decreased cardiac workload. The D4 isotope does not alter the pharmacological activity of losartan. |
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| ln Vitro |
In vitro, losartan D4 exhibits the same activity as non-deuterated losartan as an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT₁ receptors. It prevents angiotensin II from binding to the receptor, thereby inhibiting the downstream signaling cascade that leads to vasoconstriction. The D4 isotope is used as an internal standard in analytical assays.
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| ln Vivo |
In vivo, losartan D4 is used as an internal standard for pharmacokinetic studies of losartan. It is typically co-administered with losartan or spiked into biological samples to enable accurate quantification. The pharmacological effects of losartan D4 are identical to those of losartan, including blood pressure reduction, improved endothelial function, and renoprotective effects.
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| Enzyme Assay |
For in vitro receptor binding assays, losartan D4 can be evaluated for AT₁ receptor binding affinity. Radiolabeled angiotensin II (e.g., ¹²⁵I-angiotensin II) is incubated with membrane preparations containing AT₁ receptors and varying concentrations of losartan D4. Bound and free ligand are separated by filtration. IC₅₀ values are calculated from competition binding curves. The D4 isotope does not affect binding affinity.
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| Cell Assay |
For in vitro cell-based assays, losartan D4 is tested on cells expressing AT₁ receptors, such as vascular smooth muscle cells or adrenal cells. Cells are treated with the compound at various concentrations (typically 0.1 nM-10 µM) and stimulated with angiotensin II. Intracellular calcium mobilization, MAPK activation, or aldosterone production is measured as a readout of receptor activity. IC₅₀ values are determined from dose-response curves.
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| Animal Protocol |
For in vivo animal experiments, losartan D4 is typically administered orally or intravenously to rodents. Blood samples are collected at various time points, and losartan D4 levels are measured by LC-MS/MS. The compound's pharmacokinetic parameters are determined using non-compartmental analysis. Losartan D4 can also be used in pharmacodynamic studies to correlate drug exposure with blood pressure reduction.
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| ADME/Pharmacokinetics |
Losartan D4 has a molecular weight of 426.94 g/mol and formula C₂₂H₁₉D₄ClN₆O. It is soluble in DMSO (100 mM) and ethanol (100 mM). As an internal standard, it exhibits identical chromatographic and mass spectrometric behavior to losartan but can be distinguished by mass due to the 4 Da mass shift. The deuterium atoms do not significantly alter the pharmacokinetics of the compound.
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| Toxicity/Toxicokinetics |
Toxicological data for losartan D4 are limited, as it is used as an analytical standard rather than a therapeutic agent. Losartan itself is generally well-tolerated, with common adverse effects including dizziness, hyperkalemia, and hypotension. The D4 isotope is not expected to have different toxicity compared to non-deuterated losartan. The compound is classified as a research-grade reagent.
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| Additional Infomation |
Losartan D4 is a research-use only compound and has not been approved for clinical applications as a deuterated drug. It is also known as losartan-d4 and DuP-753 D4. Its molecular weight is 426.94, and its formula is C₂₂H₁₉D₄ClN₆O. The compound is used as an internal standard for the quantification of losartan in biological samples by GC- or LC-MS. It is available from various research chemical suppliers.
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| Molecular Formula |
C₂₂H₁₉D₄CLN₆O
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|---|---|
| Molecular Weight |
426.94
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| Exact Mass |
426.19
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| CAS # |
1030937-27-9
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| Related CAS # |
Losartan-d4 (carboxylic acid); 1246820-62-1; Losartan; 114798-26-4; Losartan potassium; 124750-99-8
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| PubChem CID |
25235250
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| Appearance |
White to off-white solid powder
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| LogP |
4.266
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
520
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C(C(=C1CN2C(=NC(=C2CO)Cl)CCCC)[2H])[2H])C3=CC=CC=C3C4=NNN=N4)[2H]
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| InChi Key |
PSIFNNKUMBGKDQ-IRYCTXJYSA-N
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| InChi Code |
InChI=1S/C22H23ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,30H,2-3,8,13-14H2,1H3,(H,25,26,27,28)/i9D,10D,11D,12D
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| Chemical Name |
[2-butyl-5-chloro-3-[[2,3,5,6-tetradeuterio-4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol
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| Synonyms |
DuP-753 D4; DuP753 D4; DuP 753 D4
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3422 mL | 11.7112 mL | 23.4225 mL | |
| 5 mM | 0.4684 mL | 2.3422 mL | 4.6845 mL | |
| 10 mM | 0.2342 mL | 1.1711 mL | 2.3422 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.
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