| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Sinapine thiocyanate targets acetylcholinesterase (AChE), an enzyme responsible for hydrolyzing the neurotransmitter acetylcholine in the synaptic cleft. It also targets P-glycoprotein (P-gp), a membrane transporter involved in multidrug resistance. The compound downregulates multidrug resistance 1 (MDR1) expression. Its antioxidant and anti-inflammatory activities are mediated through modulation of oxidative stress pathways and cytokine production.
|
|---|---|
| ln Vitro |
Sinapine (6 or 60 μM; 1 hour) counteracts H2O2 and antimycin A-induced mitochondrial oxidative stress in cardiomyocytes [1]. Sinapine (10-200 μM; 24 h) reduces the growth of Caco-2 cells in a dose-dependent manner with relatively moderate toxicity [3]. Sinapine (10-200 μM; 24 hours) enhances the accumulation of doxorubicin in Caco-2 cells via producing a reduction in P-glycoprotein (P-gp) [3]. Sinapine (10-200 μM; 24 hours) significantly lowers the phosphorylation of FRS2α and ERK1/2 [3].
In vitro, Sinapine thiocyanate (6 or 60 µM; 1 hour) counteracts H₂O₂- and antimycin A-induced mitochondrial oxidative stress in cardiomyocytes. It inhibits the proliferation of Caco-2 colon cancer cells in a dose-dependent manner (10-200 µM; 24 hours) with relatively low toxicity. At 10-200 µM, it promotes doxorubicin accumulation in Caco-2 cells by inducing P-gp decrease. It significantly reduces phosphorylation of FRS2α and ERK1/2. It also inhibits AChE activity with an IC50 in the micromolar range. |
| ln Vivo |
By altering the makeup of the intestinal microbiota in mice, sinapine lowers the incidence of non-alcoholic fatty liver disease [2].
In vivo, Sinapine thiocyanate reduces non-alcoholic fatty liver disease in mice by modulating the composition of the gut microbiota. Its anti-inflammatory and antioxidant properties have been demonstrated in animal models of oxidative stress. The compound exhibits radioprotective effects, suggesting potential utility in protecting against radiation-induced damage. In models of neurodegeneration, AChE inhibition may improve cholinergic transmission and cognitive function. |
| Enzyme Assay |
In vitro enzyme assays for Sinapine thiocyanate are conducted to evaluate acetylcholinesterase (AChE) inhibition. AChE activity is measured using Ellman's colorimetric method, where the enzyme hydrolyzes acetylthiocholine to produce thiocholine, which reacts with 5,5'-dithiobis-(2-nitrobenzoic acid) (DTNB) to form a yellow chromophore measured at 412 nm. The compound is incubated with AChE and substrate at varying concentrations, and IC50 values are calculated from inhibition curves.
|
| Cell Assay |
Cellular assays for Sinapine thiocyanate are performed using Caco-2 colon cancer cells and cardiomyocytes. Cells are seeded in multi-well plates and treated with compound concentrations ranging from 6 to 200 µM for 1 to 24 hours. Cell viability is assessed using MTT or CCK-8 assays. P-gp expression and function are evaluated by Western blotting and intracellular accumulation of fluorescent substrates such as rhodamine 123. Mitochondrial oxidative stress is measured using fluorescent probes such as MitoSOX or DCFH-DA.
|
| Animal Protocol |
In vivo animal studies for Sinapine thiocyanate have been conducted in mouse models of non-alcoholic fatty liver disease. Mice are administered the compound orally or intraperitoneally, and gut microbiota composition is analyzed by 16S rRNA sequencing. Liver histology, serum biomarkers (ALT, AST), and inflammatory cytokine levels are assessed. Radioprotective effects are evaluated in irradiation models. Neuroprotective efficacy is assessed in cognitive or neurodegenerative disease models.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Sinapine thiocyanate are limited. The compound has a molecular weight of 368.45 and is soluble in DMSO (≥125 mg/mL). It is likely to be absorbed following oral administration, but bioavailability may be influenced by P-gp-mediated efflux. Metabolic pathways may involve hydrolysis of the choline ester and conjugation reactions. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion.
|
| Toxicity/Toxicokinetics |
Toxicological data for Sinapine thiocyanate are limited. In vitro studies in Caco-2 cells indicate relatively low toxicity at concentrations up to 200 µM. The compound has been used in research settings without reports of significant adverse effects. Standard toxicity screening would involve acute and repeated-dose studies in rodents with evaluation of clinical signs, body weight, hematology, clinical chemistry, and histopathology.
|
| References |
|
| Additional Infomation |
Sinapine thiocyanate is an alkaloid isolated from cruciferous seeds with anti-inflammatory, antioxidant, anti-tumor, anti-angiogenic, and radioprotective activities. It inhibits acetylcholinesterase (AChE) and P-glycoprotein (P-gp). It counteracts mitochondrial oxidative stress in cardiomyocytes, inhibits Caco-2 cell proliferation, and reduces non-alcoholic fatty liver disease in mice via gut microbiota modulation. It is investigated for Alzheimer's disease, Parkinson's disease, and cancer research.
|
| Molecular Formula |
C17H24N2O5S
|
|---|---|
| Molecular Weight |
368.4479
|
| Exact Mass |
368.14
|
| CAS # |
7431-77-8
|
| Related CAS # |
Sinapine;18696-26-9;Sinapine hydroxide;122-30-5
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
1.686
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~135.70 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7141 mL | 13.5704 mL | 27.1407 mL | |
| 5 mM | 0.5428 mL | 2.7141 mL | 5.4281 mL | |
| 10 mM | 0.2714 mL | 1.3570 mL | 2.7141 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
