| 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. Unlabeled tramiprosate (homotaurine) is an orally active and brain-penetrant natural amino acid (found in red marine algae) that targets soluble amyloid-beta (Abeta) aggregates. It binds to soluble Abeta peptides and maintains them in a non-fibrillar form, preventing their assembly into neurotoxic oligomers and fibrils. Tramiprosate is also a GABA analog with neuroprotective, anticonvulsant, and antihypertensive properties.
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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].
Tramiprosate-d6 is not used for measuring intrinsic biological activity; its role is analytical. Unlabeled tramiprosate binds directly to soluble Abeta peptides, forming a stable complex that sequesters Abeta and prevents its aggregation into beta-sheet-rich fibrils. This mechanism is believed to reduce amyloid plaque burden and neurotoxicity. Tramiprosate also acts as a GABA analog, exerting neuroprotective and anticonvulsant effects through modulation of GABAergic neurotransmission. |
| ln Vivo |
Unlabeled tramiprosate has been studied in vivo in animal models of Alzheimer‘s disease and has shown efficacy in reducing amyloid-beta deposition and improving cognitive function. In transgenic mouse models, tramiprosate treatment reduces brain amyloid plaque burden and attenuates cognitive deficits. Tramiprosate also shows neuroprotective activity in models of neuronal injury. The deuterated standard is not used for in vivo activity studies but as an internal standard for PK studies.
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| Enzyme Assay |
Tramiprosate-d6 is not used in non-cellular binding assays as a test compound. For binding studies of unlabeled tramiprosate, a standard fluorescence-based aggregation assay using thioflavin T (ThT) is employed. Synthetic Abeta peptides (e.g., Abeta1-40 or Abeta1-42) are incubated with various concentrations of tramiprosate at 37degC in PBS. Thioflavin T fluorescence (excitation 440 nm, emission 485 nm) is measured over time to monitor fibril formation. A decrease in ThT fluorescence indicates inhibition of amyloid aggregation.
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| Cell Assay |
For cellular assays, primary cortical neurons or neuroblastoma cells (e.g., SH-SY5Y) are exposed to pre-aggregated Abeta peptides in the presence or absence of tramiprosate. After 24-48 hours, cell viability is assessed by MTT or LDH assays. Tramiprosate treatment should protect cells from Abeta-induced cytotoxicity by binding to soluble Abeta and preventing its aggregation into neurotoxic species. Tramiprosate (Alzhemed, 50-400 uM) is added 1 hour prior to Abeta exposure.
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| Animal Protocol |
Tramiprosate-d6 is used as an internal standard in pharmacokinetic studies of unlabeled tramiprosate. A typical protocol involves administering tramiprosate orally to rats or mice. Blood samples are collected via tail vein or cardiac puncture at multiple time points (e.g., 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 hours). A constant amount of Tramiprosate-d6 is spiked into each plasma sample as an internal standard. Following protein precipitation, samples are analyzed by LC-MS/MS to quantify unlabeled tramiprosate concentrations.
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| ADME/Pharmacokinetics |
Tramiprosate-d6 is chemically identical to the unlabeled 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. Unlabeled tramiprosate (homotaurine) is reported to have good oral bioavailability and can cross the blood-brain barrier (BBB), enabling it to reach the brain for its anti-Abeta effects. The deuterated standard is stable under standard LC-MS conditions.
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| Toxicity/Toxicokinetics |
No direct toxicological data is provided for the deuterated standard, as it is used at trace analytical levels. Unlabeled tramiprosate (Alzhemed) was evaluated in clinical trials for Alzheimer‘s disease and was generally well-tolerated. Most common adverse effects were mild-to-moderate gastrointestinal symptoms (nausea, diarrhea). Tramiprosate is a GABA analog, and at high doses, GABAergic side effects (sedation, dizziness) may occur. The deuterated standard poses negligible toxicity risk in analytical assays.
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| References |
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| Additional Infomation |
Tramiprosate-d6 is a critical analytical standard for bioanalysis of the Alzheimer's drug candidate tramiprosate. Unlabeled tramiprosate (Alzhemed, homotaurine) progressed to Phase III clinical trials for the treatment of mild-to-moderate Alzheimer‘s disease. Although the initial Phase III trial did not meet its primary endpoints, tramiprosate remains a valuable research tool for studying the role of Abeta aggregation in AD pathogenesis. The deuterated internal standard is used for NMR, GC-MS, and LC-MS quantification in pharmacokinetic and bioequivalence studies.
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| Molecular Formula |
C3H3D6NO3S
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|---|---|
| Molecular Weight |
145.21
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| Exact Mass |
145.067
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| CAS # |
1131576-06-1
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| Related CAS # |
Tramiprosate;3687-18-1
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| PubChem CID |
25253924
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.508
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| LogP |
-2.25
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
8
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| Complexity |
133
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])(C([2H])([2H])N)C([2H])([2H])S(=O)(=O)O
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| InChi Key |
SNKZJIOFVMKAOJ-NMFSSPJFSA-N
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| InChi Code |
InChI=1S/C3H9NO3S/c4-2-1-3-8(5,6)7/h1-4H2,(H,5,6,7)/i1D2,2D2,3D2
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| Chemical Name |
3-amino-1,1,2,2,3,3-hexadeuteriopropane-1-sulfonic acid
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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) |
H2O: 50 mg/mL (344.33 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 | 6.8866 mL | 34.4329 mL | 68.8658 mL | |
| 5 mM | 1.3773 mL | 6.8866 mL | 13.7732 mL | |
| 10 mM | 0.6887 mL | 3.4433 mL | 6.8866 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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