| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Not applicable. 3-Hydroxylidocaine is a drug metabolite and is not a pharmacologically active drug itself. The parent drug, lidocaine, is a voltage-gated sodium channel (Nav) blocker. 3-Hydroxylidocaine is an aromatic hydroxylation product. Its primary function is as an analytical standard for assessing lidocaine exposure. The mechanism of action of its formation is via CYP450 enzymes (mainly CYP3A4).
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|---|---|
| ln Vitro |
No pharmacological in vitro data is applicable. 3-Hydroxylidocaine is a major metabolite of lidocaine and is used as an analytical reference standard for drug metabolism and toxicology studies. Its primary activity is as a marker for the metabolic breakdown of lidocaine. Information on its in vitro potency or efficacy is not reported or relevant to its use.
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| ln Vivo |
A study in rats and sheep found that 3-Hydroxylidocaine is a major metabolite of lidocaine. The parent drug, lidocaine, is used clinically as a local anesthetic and to treat ventricular arrhythmias. The in vivo activity of the metabolite is related to the hepatic clearance of the parent drug. Its concentration in plasma is used to characterize the metabolic phenotype of the subject.
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| Enzyme Assay |
Not applicable. 3-Hydroxylidocaine is an analytical standard. A typical protocol for its use in LC-MS/MS: A calibration curve is prepared by spiking a blank biological matrix (e.g., plasma, urine) with known concentrations of 3-Hydroxylidocaine. A stable-labeled internal standard, such as 3-Hydroxylidocaine-d6, is added to all calibrators and samples. After protein precipitation or solid-phase extraction, the samples are analyzed by LC-MS/MS. The peak area ratio of the analyte to the internal standard is used for quantification.
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| Cell Assay |
Not applicable. 3-Hydroxylidocaine is an analytical standard. It is not used in cell culture as a test article for pharmacological studies. It can be spiked into cell lysates or culture media to validate an LC-MS/MS method that will be used to measure metabolite concentrations in samples from drug treatment experiments.
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| Animal Protocol |
3-Hydroxylidocaine is the major metabolite of lidocaine in rats and sheep. As an analytical standard, it is not administered to animals as a test substance. However, it can be measured in animal samples. In a typical rat PK study, animals are administered lidocaine, and blood samples are collected. The plasma is then processed and analyzed using LC-MS/MS with a calibration curve and quality controls prepared from the 3-Hydroxylidocaine standard.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known metabolites of 3-hydroxylidocaine include 3-hydroxymonoethylglycyldimethylamine. 3-hydroxylidocaine is a known metabolite of lidocaine. 3-Hydroxylidocaine is the major metabolite of lidocaine. As a metabolite, its pharmacokinetics (formation and elimination) are linked to the PK of its parent compound, lidocaine. The rate of its formation and the ratio of 3-Hydroxylidocaine to lidocaine in plasma can serve as a marker for CYP3A4 activity. As an analytical standard, it does not have a PK profile of its own. |
| Toxicity/Toxicokinetics |
No specific toxicity data was found for 3-Hydroxylidocaine. It is considered a major metabolite of lidocaine. The toxicological profile of the metabolite is not well characterized; however, accumulation of this or other metabolites of lidocaine could be related to the central nervous system (CNS) and cardiovascular toxicities seen with lidocaine overdose. As an analytical standard, it is handled in very small amounts.
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| References | |
| Additional Infomation |
3-Hydroxylidocaine is an amino acid amide and a metabolite of lidocaine.
3-Hydroxylidocaine (CAS: 34604-55-2) has a molecular formula of C14H22N2O2 and a molecular weight of 250.34. Its IUPAC name is 2-(diethylamino)-N-(3-hydroxy-2,6-dimethylphenyl)acetamide. It is the major metabolite of lidocaine in rats and sheep and is used as an analytical standard for research purposes. |
| Molecular Formula |
C14H22N2O2
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|---|---|
| Molecular Weight |
250.34
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| Exact Mass |
250.168
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| CAS # |
34604-55-2
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| PubChem CID |
161824
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| Appearance |
Typically exists as solids at room temperature
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| Density |
1.103g/cm3
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| Boiling Point |
390.8ºC at 760 mmHg
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| Flash Point |
190.2ºC
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| Index of Refraction |
1.569
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| LogP |
2.362
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N(CC)CC(NC1C(C)=CC=C(O)C=1C)=O)C
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| InChi Key |
PMGUCIDDSCRAMY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H22N2O2/c1-5-16(6-2)9-13(18)15-14-10(3)7-8-12(17)11(14)4/h7-8,17H,5-6,9H2,1-4H3,(H,15,18)
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| Chemical Name |
2-(diethylamino)-N-(3-hydroxy-2,6-dimethylphenyl)acetamide
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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 | 3.9946 mL | 19.9728 mL | 39.9457 mL | |
| 5 mM | 0.7989 mL | 3.9946 mL | 7.9891 mL | |
| 10 mM | 0.3995 mL | 1.9973 mL | 3.9946 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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