| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg | |||
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| Targets |
The primary target of Losartan D4 Carboxylic Acid is the angiotensin II receptor type 1 (AT1), a G protein-coupled receptor that mediates the vasoconstrictor and aldosterone-secreting effects of angiotensin II. Losartan carboxylic acid (EXP3174) is a potent and selective antagonist of the AT1 receptor, with Ki values of 0.97 nM for rat AT1B, 0.57 nM for rat AT1A, and 0.67 nM for human AT1. By blocking the AT1 receptor, the compound inhibits the renin-angiotensin-aldosterone system (RAAS), leading to vasodilation, reduced aldosterone secretion, and decreased blood pressure. The deuterated form, Losartan D4 Carboxylic Acid, is chemically identical to the non-deuterated metabolite but is used as an analytical standard.
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| ln Vitro |
Losartan D4 Carboxylic Acid is not typically evaluated for in vitro pharmacological activity, as its primary use is as an analytical standard. However, the non-deuterated metabolite, losartan carboxylic acid, is a potent AT1 receptor antagonist with Ki values in the sub-nanomolar range. It inhibits angiotensin II-induced vasoconstriction and aldosterone secretion. The deuterated compound is expected to have the same pharmacological activity as the non-deuterated form, but its use is primarily analytical.
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| ln Vivo |
Losartan D4 Carboxylic Acid is not used in vivo as a therapeutic agent; it is an analytical standard. The non-deuterated metabolite, losartan carboxylic acid, is the active form of losartan and is responsible for the drug's antihypertensive effects in vivo. It is administered as the prodrug losartan, which is converted to the active metabolite in the liver. The deuterated compound is used in pharmacokinetic studies to accurately quantify losartan and its metabolites in biological samples.
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| Enzyme Assay |
In vitro enzyme assays are not typically performed for Losartan D4 Carboxylic Acid, as it is an analytical standard. However, its identity and purity can be confirmed by HPLC, NMR, and MS. Its use in analytical methods involves spiking it into biological samples as an internal standard for LC-MS/MS analysis.
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| Cell Assay |
In vitro cell-based assays are not typically performed for Losartan D4 Carboxylic Acid. As an analytical standard, its primary use is in the quantification of losartan and its metabolites. Its effects on cell signaling or viability are not standard assays for this compound.
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| Animal Protocol |
In vivo animal studies are not typically conducted with Losartan D4 Carboxylic Acid. It is used as an internal standard in pharmacokinetic studies to quantify losartan and its metabolites in plasma and tissues from animals dosed with losartan. The deuterated compound corrects for matrix effects, extraction recovery, and ionization efficiency, ensuring accurate quantification.
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| ADME/Pharmacokinetics |
Losartan D4 Carboxylic Acid has a molecular weight of 440.92 g/mol and a molecular formula of C₂₂H₁₇D₄ClN₆O₂. The deuterium labeling provides a mass shift of 4 Da compared to the non-deuterated compound, allowing for its use as an internal standard in mass spectrometry. It is supplied as an off-white to light yellow solid powder with a purity of ≥98%. It should be stored as a powder at -20°C for up to three years.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for Losartan D4 Carboxylic Acid. As a deuterated compound used as an internal standard, it is typically handled in very small quantities. The safety profile of losartan and its metabolites is well-established from clinical use. For laboratory handling, standard safety precautions for research chemicals should be observed. The compound is intended for research use only and is not for human therapeutic or diagnostic use.
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| Additional Infomation |
Losartan D4 Carboxylic Acid is a deuterium-labeled form of losartan carboxylic acid (EXP3174), the active metabolite of losartan. It has a molecular formula of C₂₂H₁₇D₄ClN₆O₂ and a molecular weight of 440.92 g/mol. The compound is used as an internal standard for the quantification of losartan and its metabolites in biological samples by LC-MS/MS. It is an angiotensin II receptor antagonist. Losartan D4 Carboxylic Acid is for research use only.
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| Molecular Formula |
C₂₂H₁₇D₄CLN₆O₂
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|---|---|
| Molecular Weight |
440.92
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| Exact Mass |
440.17
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| CAS # |
1246820-62-1
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| Related CAS # |
Losartan Carboxylic Acid; 124750-92-1; Losartan; 114798-26-4; Losartan potassium; 124750-99-8; Losartan-d4; 1030937-27-9
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| PubChem CID |
45359014
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.472
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
590
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C(C(=C1CN2C(=NC(=C2C(=O)O)Cl)CCCC)[2H])[2H])C3=CC=CC=C3C4=NNN=N4)[2H]
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| InChi Key |
ZEUXAIYYDDCIRX-IRYCTXJYSA-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)/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]imidazole-4-carboxylic acid
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| Synonyms |
E-3174; D4E3174; D4EXP-3174; D4 E-3174; EXP 3174 E 3174EXP3174
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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 | 2.2680 mL | 11.3399 mL | 22.6799 mL | |
| 5 mM | 0.4536 mL | 2.2680 mL | 4.5360 mL | |
| 10 mM | 0.2268 mL | 1.1340 mL | 2.2680 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.
Products are for research use only; We do not sell to patients
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