| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Not applicable for the deuterated internal standard. Unlabeled oxprenolol is a non-selective beta-adrenergic receptor (beta-AR) antagonist that also possesses intrinsic sympathomimetic activity (ISA) and membrane stabilizing effects. It competes with catecholamines for binding at beta1 and beta2 adrenergic receptors, with binding affinity (Ki) reported in the nanomolar range.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Oxprenolol-d7 is not used for measuring intrinsic biological activity; its role is analytical. Unlabeled oxprenolol is a non-selective beta-blocker that competitively antagonizes catecholamines at beta1 and beta2 adrenergic receptors. In functional assays, oxprenolol blocks the positive chronotropic effects of isoprenaline in isolated rabbit atria, demonstrating its beta-adrenoceptor antagonist activity. |
| ln Vivo |
Oxprenolol-d7 itself is not used for in vivo activity studies. Unlabeled oxprenolol is clinically approved in Europe for the treatment of hypertension and angina pectoris. It also shows some utility for the treatment of anxiety. Oxprenolol reduces plasma renin activity (PRA) and mean blood pressure in animal models and prevents the stimulatory effects of isoproterenol on renin release and heart rate.
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| Enzyme Assay |
Oxprenolol-d7 is not used in non-cellular binding assays as a test compound. For binding studies, a standard protocol uses [3H]oxprenolol or other radiolabeled beta-antagonists. Membrane preparations from cells expressing human beta-adrenergic receptors are incubated with the radioligand and varying concentrations of unlabeled competitor. Bound radioactivity is separated by filtration through glass fiber filters and measured by liquid scintillation counting to calculate Ki values.
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| Cell Assay |
No standard cell-based protocol is applicable for Oxprenolol-d7 as an internal standard. For functional characterization of unlabeled oxprenolol, HEK-293 cells expressing human beta1 or beta2 adrenoceptors are used. Cells are pre-treated with forskolin to stimulate cAMP production, then treated with isoproterenol to activate the receptors. Oxprenolol is added to compete with isoproterenol, and intracellular cAMP levels are measured by HTRF or ELISA to determine antagonist potency.
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| Animal Protocol |
No in vivo protocol is applicable for Oxprenolol-d7 as an internal standard. For pharmacokinetic studies, unlabeled oxprenolol is administered to rats or human subjects (oral or intravenous). Blood or plasma samples are collected at various time points post-dose, and a constant known amount of Oxprenolol-d7 hydrochloride is spiked into each sample as an internal standard before LC-MS/MS analysis for quantification of unlabeled oxprenolol.
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| ADME/Pharmacokinetics |
Oxprenolol-d7 hydrochloride is chemically identical to the unlabeled analyte except for a +7 Da mass shift due to seven deuterium atoms, resulting in virtually identical extraction recovery, chromatographic retention time, and ionization efficiency. It is stable under standard LC-MS conditions. Unlabeled oxprenolol undergoes extensive first-pass metabolism, with only 30% of an oral dose reaching systemic circulation.
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| Toxicity/Toxicokinetics |
No direct toxicological data is provided for Oxprenolol-d7 hydrochloride, as it is used at trace analytical levels. Unlabeled oxprenolol has a well-characterized clinical safety profile; common adverse effects include bradycardia, hypotension, fatigue, and gastrointestinal disturbances. The intrinsic sympathomimetic activity of oxprenolol may reduce the risk of resting bradycardia compared to other beta-blockers.
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| References |
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| Additional Infomation |
Oxprenolol-d7 hydrochloride is a critical analytical standard for pharmacokinetic and bioequivalence studies. Unlabeled oxprenolol (Trasicor, Slow-Trasicor) is a clinically approved beta-blocker developed by Novartis/Ciba-Geigy and is approved for use in many countries outside the United States. Its combination of non-selective beta-blockade with intrinsic sympathomimetic activity distinguishes it from other beta-blockers such as propranolol.
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| Molecular Formula |
C15H17D7CLNO3
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|---|---|
| Molecular Weight |
308.85
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| Exact Mass |
308.188
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| CAS # |
1189649-47-5
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| Related CAS # |
Oxprenolol hydrochloride;6452-73-9
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| PubChem CID |
46782657
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| Appearance |
White to off-white solid powder
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| LogP |
3.182
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
20
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| Complexity |
246
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])C([2H])(C([2H])([2H])[2H])NCC(COC1=CC=CC=C1OCC=C)O.Cl
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| InChi Key |
COAJXCLTPGGDAJ-CXUOUXNTSA-N
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| InChi Code |
InChI=1S/C15H23NO3.ClH/c1-4-9-18-14-7-5-6-8-15(14)19-11-13(17)10-16-12(2)3;/h4-8,12-13,16-17H,1,9-11H2,2-3H3;1H/i2D3,3D3,12D;
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| Chemical Name |
1-(1,1,1,2,3,3,3-heptadeuteriopropan-2-ylamino)-3-(2-prop-2-enoxyphenoxy)propan-2-ol;hydrochloride
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2378 mL | 16.1891 mL | 32.3782 mL | |
| 5 mM | 0.6476 mL | 3.2378 mL | 6.4756 mL | |
| 10 mM | 0.3238 mL | 1.6189 mL | 3.2378 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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