| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
| Targets |
The primary target of Tramiprosate is amyloid-beta (Aβ), a peptide that forms neurotoxic plaques in the brains of patients with Alzheimer's disease. By binding to soluble Aβ, tramiprosate prevents its aggregation and the formation of plaques. This reduces neurotoxicity and may slow the progression of Alzheimer's disease. The compound also has effects on the GABAergic system, as it is a structural analog of GABA.
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| ln Vitro |
In PC12 cells and primary cortical neurons, hypoxia/glucose deprivation (OGD) or NMDA-induced NGF differentiation is considerably attenuated by trimiprosate (200 μg/mL, 40 μg/mL, 8 μg/mL, and 1.6 μg/mL; 1 hour). Tramiprosate suppresses the translocation of nNOS from the cytoplasm to the membrane as well as the intensity of the interaction between nNOS and PSD95 [1].
In vitro, tramiprosate has been shown to bind to soluble amyloid-beta (Aβ) and prevent its aggregation. It inhibits the formation of Aβ fibrils and reduces neurotoxicity in neuronal cell cultures. The compound's effects on Aβ aggregation have been confirmed in various in vitro models. |
| ln Vivo |
After MCAO, trimiprost (6.25–50 mg/kg; intraperitoneally; once) decreases infarct volume in a dose-dependent manner. Treatment with trimiprost (50 mg/kg) significantly improves neurological function [1].
In vivo, tramiprosate has been studied in clinical trials for the treatment of Alzheimer's disease. It has been shown to reduce the levels of Aβ in the brain and to improve cognitive function in some studies. However, the results of clinical trials have been mixed, and the compound is not currently approved for the treatment of Alzheimer's disease. |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for tramiprosate involve studying its binding to amyloid-beta (Aβ). The binding affinity can be measured using surface plasmon resonance (SPR) or fluorescence spectroscopy. The inhibition of Aβ aggregation can be assessed using thioflavin T fluorescence or other aggregation assays.
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| Cell Assay |
In vitro cell-based assays for tramiprosate are performed using neuronal cell lines. Cells are treated with the compound, and the protection against Aβ-induced neurotoxicity is assessed by measuring cell viability. The compound's effects on Aβ aggregation and neurotoxicity are evaluated.
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| Animal Protocol |
Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rats (200-250 g) undergoing middle cerebral artery occlusion (MCAO) [1]
Doses: 50 mg/kg, 25 mg/kg, 12.5 mg/kg, or 6.25 mg/kg administered Methods: intraperitoneal (ip) injection; Experimental Results: Infarct volume diminished in a dose-dependent manner after MCAO. In vivo animal experiments for tramiprosate are conducted using transgenic mouse models of Alzheimer's disease. The compound is administered orally, and its effects on Aβ levels, plaque formation, and cognitive function are assessed. These studies confirm the compound's ability to reduce Aβ pathology and improve cognitive function. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tramiprosate indicate that it is orally active. The compound has a molecular weight of 139.17 and a molecular formula of C3H9NO3S. It is a solid at room temperature. The compound is well-absorbed and crosses the blood-brain barrier. It is metabolized in the liver and excreted renally. Its half-life is approximately 2-4 hours.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tramiprosate indicate that it is generally well-tolerated. Common side effects may include nausea, vomiting, and diarrhea. The compound may also cause dizziness and headache. Long-term safety data are being evaluated in ongoing studies.
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| References |
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| Additional Infomation |
3-Aminopropanesulfonic acid is an aminosulfonic acid, a 3-amino derivative of propanesulfonic acid. It is an algal metabolite with nootropic, anticonvulsant, GABA agonist, and anti-inflammatory effects. It is the zwitterionic tautomer of 3-aminopropanesulfonic acid.
Drug Indications It has been studied for the treatment of stroke and Alzheimer's disease. Other information: Tramiprosate is also known as 3-amino-1-propanesulfonic acid and homotaurine. It has been investigated for the treatment of Alzheimer's disease. The compound binds to soluble amyloid-beta and prevents its aggregation. Its CAS number is 3687-18-1. |
| Molecular Formula |
C3H9NO3S
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| Molecular Weight |
139.17
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| Exact Mass |
139.03
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| CAS # |
3687-18-1
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| Related CAS # |
Tramiprosate-d6;1131576-06-1
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| PubChem CID |
1646
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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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| Melting Point |
293 °C (dec.)(lit.)
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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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| InChi Key |
SNKZJIOFVMKAOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C3H9NO3S/c4-2-1-3-8(5,6)7/h1-4H2,(H,5,6,7)
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| Chemical Name |
3-aminopropane-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 : ~20 mg/mL (~143.71 mM)
DMSO : ~1 mg/mL (~7.19 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 140 mg/mL (1005.96 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.1855 mL | 35.9273 mL | 71.8546 mL | |
| 5 mM | 1.4371 mL | 7.1855 mL | 14.3709 mL | |
| 10 mM | 0.7185 mL | 3.5927 mL | 7.1855 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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