| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Olmesartan D4 targets the angiotensin II receptor type 1 (AT1R) as an antagonist. The deuterium labeling does not significantly alter the pharmacological properties of olmesartan. Olmesartan is an AT1R antagonist used to treat high blood pressure. The D4 analog is used in pharmacokinetic analysis as an internal standard.
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|---|---|
| ln Vitro |
In vitro, olmesartan D4 exhibits the same pharmacological activity as unlabeled olmesartan, acting as an AT1R antagonist. However, the primary use of the D4 analog is as an analytical standard rather than for pharmacological studies. Olmesartan is a potent AT1R antagonist. The D4 analog is used in receptor binding assays as a reference standard.
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| ln Vivo |
In vivo, olmesartan D4 is not typically used for pharmacological studies but rather as an internal standard for measuring olmesartan levels in biological samples. The deuterium-labeled compound behaves similarly to unlabeled olmesartan in vivo. Olmesartan is used clinically as an antihypertensive agent. The D4 analog is used in pharmacokinetic studies to track olmesartan levels.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for olmesartan D4 typically involve competition binding studies using membranes from cells expressing human AT1 receptors. The compound is incubated with various concentrations of radiolabeled ligand in binding buffer. Nonspecific binding is determined in the presence of excess unlabeled olmesartan. Following incubation, bound and free ligand are separated by filtration, and bound radioactivity is measured. Competition curves are generated, and IC₅₀ or Kᵢ values are calculated.
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| Cell Assay |
In vitro cell-based assays for olmesartan D4 are not typically performed, as it is primarily used as an analytical standard. However, the unlabeled olmesartan is studied in cell lines expressing AT1 receptors. Cells are treated with olmesartan, and receptor signaling is assessed by measuring downstream effects such as cAMP accumulation or calcium mobilization. The D4 analog would be expected to have identical effects to unlabeled olmesartan.
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| Animal Protocol |
In vivo animal studies with olmesartan D4 are not typically performed, as it is primarily used as an analytical standard. The unlabeled olmesartan is extensively studied in animal models of hypertension. Olmesartan is administered to rodents via various routes, and blood pressure is measured. The D4 analog is used in pharmacokinetic studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of olmesartan D4 are identical to those of unlabeled olmesartan. The compound is used as an internal standard in PK studies to quantify olmesartan levels in biological samples. Olmesartan is an orally active AT1R antagonist used for hypertension. The D4 analog is used to correct for matrix effects and ion suppression in mass spectrometry analysis.
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| Toxicity/Toxicokinetics |
The toxicity profile of olmesartan D4 is identical to that of unlabeled olmesartan. Olmesartan has well-characterized safety and tolerability profiles as an antihypertensive agent. The compound is not intended for therapeutic use in the D4 form. The D4 analog is used only in small quantities as an analytical standard.
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| Additional Infomation |
Olmesartan D4 is a deuterium-labeled analytical standard used primarily in mass spectrometry as an internal standard for quantifying olmesartan concentrations. It is an angiotensin II receptor (AT1R) antagonist. The compound is used for isotope tracing, analytical method development, and quality control. It is not an approved therapeutic drug and is intended for research and analytical applications only. Synonyms include Olmesartan-d4 and RNH-6270-d4.
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| Molecular Formula |
C24H22D4N6O3
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|---|---|
| Molecular Weight |
450.5263
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| Exact Mass |
450.232
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| CAS # |
1420880-41-6
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| Related CAS # |
Olmesartan;144689-24-7;Olmesartan medoxomil;144689-63-4
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| PubChem CID |
71479812
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.656
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
656
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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)C(C)(C)O)CCC)[2H])[2H])C3=CC=CC=C3C4=NNN=N4)[2H]
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| InChi Key |
VTRAEEWXHOVJFV-ZGAVCIBUSA-N
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| InChi Code |
InChI=1S/C24H26N6O3/c1-4-7-19-25-21(24(2,3)33)20(23(31)32)30(19)14-15-10-12-16(13-11-15)17-8-5-6-9-18(17)22-26-28-29-27-22/h5-6,8-13,33H,4,7,14H2,1-3H3,(H,31,32)(H,26,27,28,29)/i10D,11D,12D,13D
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| Chemical Name |
5-(2-hydroxypropan-2-yl)-2-propyl-3-[[2,3,5,6-tetradeuterio-4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
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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 | 2.2196 mL | 11.0980 mL | 22.1961 mL | |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2196 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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