| 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 |
As a stable isotope-labeled internal standard, Pyridostigmine-d6 bromide does not have a primary pharmacological target in bioanalytical contexts. The unlabeled parent compound, pyridostigmine bromide, is a reversible inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), used clinically as a parasympathomimetic agent.
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| ln Vitro |
The unlabeled pyridostigmine reversibly inhibits acetylcholinesterase (AChE) at the neuromuscular junction, thereby increasing the concentration of acetylcholine. This in vitro activity leads to improved cholinergic transmission. The deuterated standard is not used to measure intrinsic biological activity but to quantify the parent drug.
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| ln Vivo |
In vivo, unlabeled pyridostigmine is used clinically to treat myasthenia gravis and as a pre-exposure antidote to chemical warfare nerve agents. It improves muscle strength by prolonging the action of acetylcholine at nicotinic receptors. The deuterated form is not used in vivo but serves as an analytical standard for measuring drug concentrations in patient or animal samples.
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| Enzyme Assay |
Pyridostigmine-d6 bromide is not used in non-cellular enzyme assays as a test compound. Instead, it is used as an internal standard in enzyme assays for quantification. A known, fixed amount of the deuterated internal standard is spiked into a biological sample containing unlabeled pyridostigmine. The sample is processed by protein precipitation or solid-phase extraction and analyzed by LC-MS/MS.
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| Cell Assay |
No cell-based experiments are performed with the deuterated standard. For studying the pharmacology of the unlabeled parent, cells expressing acetylcholinesterase (e.g., neuroblastoma cells or erythrocyte lysates) are used. The cells/lysates are incubated with varying concentrations of pyridostigmine, and the residual AChE activity is measured spectrophotometrically using a chromogenic substrate like acetylthiocholine, which is hydrolyzed to produce a yellow color detected at 412 nm.
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| Animal Protocol |
Pyridostigmine-d6 bromide is used as an internal standard in pharmacokinetic studies. A typical protocol involves administering unlabeled pyridostigmine bromide to rats or humans via oral or intravenous routes. Plasma samples are collected at various time points, and a constant amount of Pyridostigmine-d6 bromide is spiked into each sample as an internal standard. Samples are then processed and analyzed by LC-MS/MS to determine the concentration of the unlabeled drug.
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| ADME/Pharmacokinetics |
Pyridostigmine-d6 bromide is chemically identical to the analyte except for a +6 Da mass shift due to six deuterium atoms, resulting in virtually identical extraction recovery, chromatographic retention time, and ionization efficiency. This stable isotope-labeled standard is stable under typical LC-MS conditions and is not susceptible to significant isotope exchange.
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| Toxicity/Toxicokinetics |
No direct toxicological data is provided for the deuterated standard, as it is used at trace analytical levels. The unlabeled pyridostigmine bromide has a well-characterized safety profile; its primary side effects are cholinergic in nature, including gastrointestinal disturbances (nausea, diarrhea), muscle cramps, and excessive salivation, due to its mechanism of reversible acetylcholinesterase inhibition.
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| Additional Infomation |
Pyridostigmine-d6 bromide is a critical tool for bioanalytical method validation and therapeutic drug monitoring. The use of a stable isotope-labeled internal standard is essential for meeting FDA and EMA guidelines for bioanalytical method validation, as it provides the highest level of accuracy and precision for quantifying drug concentrations in complex biological matrices, especially for drugs like pyridostigmine that are used in narrow therapeutic index indications.
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| Molecular Formula |
C9H13BRN2O2
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|---|---|
| Molecular Weight |
267.152691602707
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| Exact Mass |
266.053
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| CAS # |
2375858-08-3
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| Related CAS # |
Pyridostigmine bromide;101-26-8
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| PubChem CID |
71751887
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
183
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Br-].O(C(N(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)C1=CC=C[N+](C)=C1
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| InChi Key |
VNYBTNPBYXSMOO-TXHXQZCNSA-M
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| InChi Code |
InChI=1S/C9H13N2O2.BrH/c1-10(2)9(12)13-8-5-4-6-11(3)7-8;/h4-7H,1-3H3;1H/q+1;/p-1/i1D3,2D3;
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| Chemical Name |
(1-methylpyridin-1-ium-3-yl) N,N-bis(trideuteriomethyl)carbamate;bromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 50 mg/mL (187.16 mM)
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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 | 3.7432 mL | 18.7161 mL | 37.4322 mL | |
| 5 mM | 0.7486 mL | 3.7432 mL | 7.4864 mL | |
| 10 mM | 0.3743 mL | 1.8716 mL | 3.7432 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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