| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Not applicable for the deuterated internal standard. The unlabeled parent compound carazolol is a beta-adrenergic receptor (beta-AR) ligand, binding to beta1, beta2, and beta3-adrenergic receptors with Kd values of 0.2, 0.03, and 4.47 nM, respectively. Carazolol is a high-affinity antagonist at beta1/beta2 receptors but exhibits agonist activity at beta3-adrenoceptors.
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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].
Carazolol-d7 is not used for measuring intrinsic biological activity; its role is analytical. The unlabeled compound carazolol is a high-affinity beta-adrenergic receptor ligand. [3H](+/-)-Carazolol binding to membrane vesicles from canine ventricular myocardium and lung is saturable, of high affinity, and displaceable by beta-adrenergic agents in accordance with their known pharmacological potencies, confirming its utility as a radioligand for receptor characterization. |
| ln Vivo |
Carazolol-d7 itself is not used for in vivo activity studies. Unlabeled carazolol is clinically used as a beta-blocker for the treatment of hypertension. Carazolol acts as a potent competitive antagonist at beta1 and beta2 adrenoceptors, reducing heart rate and cardiac output. Its affinity for beta3-adrenoceptors has been characterized in transfected cell lines.
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| Enzyme Assay |
Carazolol-d7 is not used in non-cellular binding assays as a test compound. For binding studies, a standard protocol uses [3H](+/-)-carazolol as a radioligand. Membrane preparations (e.g., from canine ventricular myocardium) are incubated with [3H]carazolol and varying concentrations of unlabeled competitor. Bound and free radioligand are separated by filtration through glass fiber filters, and retained radioactivity is measured by liquid scintillation counting.
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| Cell Assay |
No standard cell-based protocol is applicable for Carazolol-d7 as an internal standard. For functional characterization of unlabeled carazolol, cells expressing recombinant beta-adrenergic receptors (e.g., CHO cells) are used. Intracellular cAMP accumulation is measured by HTRF after forskolin stimulation. Carazolol inhibits cAMP production in cells expressing beta1 or beta2 receptors, but stimulates cAMP in cells expressing beta3 receptors, demonstrating its antagonist vs. agonist pharmacology.
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| Animal Protocol |
No in vivo protocol is applicable for Carazolol-d7 as an internal standard. Unlabeled carazolol is administered orally or intravenously to animal models (e.g., rats or dogs) for pharmacokinetic or pharmacodynamic studies. Blood samples are collected at various time points, and Carazolol-d7 is spiked into each sample as an internal standard before LC-MS/MS analysis to quantify unlabeled drug concentrations.
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| ADME/Pharmacokinetics |
Carazolol-d7 is chemically identical to the analyte except for a +7 Da mass shift due to deuterium substitution, resulting in virtually identical extraction recovery, chromatographic retention time, and ionization efficiency. It is stable under standard LC-MS conditions. As an internal standard for bioanalysis, it provides accurate normalization for matrix effects and extraction losses in quantitative assays.
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| Toxicity/Toxicokinetics |
No direct toxicological data is provided for Carazolol-d7, as it is used at trace analytical levels. Unlabeled carazolol is a potent beta-adrenergic antagonist; potential adverse effects at high doses include bradycardia, hypotension, bronchospasm, and central nervous system depression. The deuterated internal standard poses negligible toxicity risk when used as intended in analytical assays.
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| References | |
| Additional Infomation |
Carazolol-d7 is a critical quality control tool for pharmacokinetic studies and residue monitoring. Deuterated internal standards like Carazolol-d7 are required by regulatory guidelines (FDA/EMA) for bioanalytical method validation to ensure accuracy and precision. The compound is used for quantitative analysis of carazolol in animal tissues and water samples, supporting veterinary drug safety and environmental monitoring.
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| Molecular Formula |
C18H15D7N2O2
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|---|---|
| Molecular Weight |
305.42
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| Exact Mass |
305.212
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| CAS # |
1173021-02-7
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| Related CAS # |
Carazolol;57775-29-8
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| PubChem CID |
71312455
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
531.2±40.0 °C at 760 mmHg
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| Flash Point |
275.1±27.3 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
3.59
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
350
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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=CC2=C1C3=CC=CC=C3N2)O
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| InChi Key |
BQXQGZPYHWWCEB-QLWPOVNFSA-N
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| InChi Code |
InChI=1S/C18H22N2O2/c1-12(2)19-10-13(21)11-22-17-9-5-8-16-18(17)14-6-3-4-7-15(14)20-16/h3-9,12-13,19-21H,10-11H2,1-2H3/i1D3,2D3,12D
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| Chemical Name |
1-(9H-carbazol-4-yloxy)-3-(1,1,1,2,3,3,3-heptadeuteriopropan-2-ylamino)propan-2-ol
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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 | 3.2742 mL | 16.3709 mL | 32.7418 mL | |
| 5 mM | 0.6548 mL | 3.2742 mL | 6.5484 mL | |
| 10 mM | 0.3274 mL | 1.6371 mL | 3.2742 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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