| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Berberine-d6 chloride targets multiple molecular pathways. The parent compound berberine chloride targets DNA topoisomerase, inducing ROS generation and DNA damage. It also activates AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis, making it relevant for metabolic disorder research. Additionally, berberine has been shown to modulate the NF-kappaB pathway, autophagy, and bacterial cell components. The deuterated version retains the same target interactions as non-labeled berberine, as the labeling does not alter its basic pharmacological properties.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
In vitro, berberine chloride, the parent compound, exhibits potent activity against various cancer cell lines by inducing ROS generation and DNA topoisomerase inhibition. It has been shown to inhibit the growth of human colorectal adenocarcinoma cells in both in vitro and in vivo models. Berberine also activates AMPK, leading to metabolic effects such as improved insulin sensitivity. Berberine-d6 chloride is primarily used as an analytical standard rather than for functional assessments in vitro, so specific EC50 values are not detailed for the labeled version. However, stable heavy isotope labeling does not alter biological activity. |
| ln Vivo |
Berberine-d6 chloride is not typically used in in vivo functional studies as a therapeutic agent, as it is an analytical standard for quantifying berberine levels. The parent compound berberine chloride has been extensively studied in vivo in animal models for its anti-diabetic, anti-obesity, and anti-cancer effects. For example, it inhibits the growth of human colorectal adenocarcinoma in mouse xenograft models. Berberine-d6 is used as an internal standard in animal pharmacokinetic studies to accurately trace berberine distribution and metabolism.
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| Enzyme Assay |
Binding studies for berberine-d6 chloride are not typically performed separately from those of non-labeled berberine chloride. Binding to DNA topoisomerase can be assessed using enzymatic assays that measure inhibition of DNA relaxation or supercoiling. AMPK activation is typically measured using cell-based assays rather than direct binding assays, as AMPK is activated by phosphorylation rather than direct ligand binding. The deuterated form is used as an analytical standard in these studies for quantification purposes.
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| Cell Assay |
In vitro cellular experiments for berberine-d6 chloride are not typically performed, as it is an analytical standard. However, the parent compound berberine chloride is used in a wide range of cell-based assays. Cancer cell lines (e.g., colorectal cancer cells) are treated with varying concentrations of berberine chloride. Endpoints include measurement of ROS generation using fluorescent dyes such as DCFH-DA, assessment of DNA damage by comet assay or gammaH2AX staining, evaluation of AMPK activation by immunoblotting for phospho-AMPK, determination of cell viability by MTT assay, and quantification of apoptosis by Annexin V/PI staining. For the deuterated version, specific assays are not standard.
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| Animal Protocol |
Animal protocols for berberine-d6 chloride are typically part of pharmacokinetic or metabolism studies. The compound is administered to rodents (e.g., rats or mice) at specified doses (e.g., 10-50 mg/kg) by oral gavage or intravenous injection. Blood samples are collected at various time points post-dose, and plasma concentrations are measured by LC-MS/MS. The deuterated compound serves as the internal standard to correct for matrix effects and improve quantification accuracy. For tissue distribution studies, organs such as liver, kidney, and intestines are collected and processed for analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for berberine-d6 chloride are not separately reported, as it is used as an internal standard for the quantification of non-labeled berberine. Berberine chloride itself has low oral bioavailability due to poor absorption and extensive first-pass metabolism. Deuteration can potentially alter the pharmacokinetic and metabolic profiles of drugs, though this is not specifically characterized for berberine-d6. The labeled version is stable and does not undergo significant deuterium-hydrogen exchange under physiological conditions. It is used to improve accuracy in drug development studies.
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| Toxicity/Toxicokinetics |
Toxicological data for berberine-d6 chloride are not extensively reported, as it is an analytical standard used at very low concentrations. The parent compound berberine chloride has been studied for its safety profile; it is generally considered safe at therapeutic doses, though high doses can cause gastrointestinal side effects, hepatotoxicity, and potential drug-drug interactions via CYP enzyme inhibition. As a stable isotope-labeled compound, berberine-d6 chloride does not pose additional toxicological risks beyond those of the non-labeled compound. Standard laboratory chemical safety precautions apply.
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| References | |
| Additional Infomation |
Berberine-d6 chloride (Natural Yellow 18-d6 chloride) has the molecular formula C20H12D6ClNO4 and a molecular weight of 377.85. The unlabeled berberine chloride has a CAS number of 633-65-8. Berberine is a natural isoquinoline alkaloid found in Hydrastis canadensis L. and other Berberidaceae plants. It is an AMPK activator used in research on non-alcoholic fatty liver disease (NAFLD), diabetes, and cancer. The deuterated form is used as an internal standard for the quantification of berberine in biological samples by LC-MS/MS. The compound is for research use only and not for human therapy.
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| Molecular Formula |
C20H12D6CLNO4
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| Molecular Weight |
377.85
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| Related CAS # |
Berberine chloride;633-65-8
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| Appearance |
Typically exists as solid at room temperature
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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 | 2.6466 mL | 13.2328 mL | 26.4655 mL | |
| 5 mM | 0.5293 mL | 2.6466 mL | 5.2931 mL | |
| 10 mM | 0.2647 mL | 1.3233 mL | 2.6466 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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