Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
hAChE 0.076 μM (IC50) hBACE-1 0.23 μM (IC50) hBCHE 1.204 μM (IC50)
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ln Vitro |
In SH-SY5Y, hAChE/hBACE-1-IN-1 (10-80 μM, 48 h) is safe at the highest concentration [1].
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ln Vivo |
In a mouse paradigm of scopolamine-induced cognitive impairments, hAChE/hBACE-1-IN-1 (2.5–10 mg/kg, oral, 14 days) decreases RTL and open-arm duration while improving learning and memory [1]. With no adverse effects on the brain, liver, kidneys, or heart, hAChE/hBACE-1-IN-1 (500 mg/kg, oral, 14 days) was well tolerated and non-toxic to mice [1]. In a mouse model of scopolamine induced hippocampus and cortical brain homogenates, hAChE/hBACE-1-IN-1 (10 mg/kg, PO, 14 days) crosses the blood-brain barrier and decreases AChE levels or substrates. It could lower levels of pro-inflammatory cytokines and postpone oxidative stress [1]. hAChE/hBACE-1-IN-1 (10 mg/kg, oral, 14 days) preserves brain tissue in several brain regions and suppresses BACE-1, Aβ, APP/Aβ, and tau protein in an Aβ-induced model [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y Tested Concentrations: 10 μM, 20 μM, 40 μM, 80 μM Incubation Duration: 48 h, 72 h Experimental Results: Indicated the similar in safety to donepezil at a maximum 80 μM concentration. Restored the cell that Aβ1-42 treated viability to 70% after 48 h, to 77% after 72 h cell. |
Animal Protocol |
Animal/Disease Models: scopolamine-induced amnesia models in Swiss albino mice[1].
Doses: 2.5, 5, 10 mg/kg/day Route of Administration: oral administration (po) 14 days Experimental Results: Improved learning and memory and reduce RTL and time spent in open arms. Crossed the blood-brain barrier, and decreased AChE levels or substrate hydrolysis in hippocampal and cortex brain homogenates. decreased MDA, ROS levels, nitrite concentration, and increased GSH levels in a dose-dependent manner. decreased levels of proinflammatory cytokines. Animal/Disease Models: Aβ-induced models in Swiss albino mice[1]. Doses: 10 mg/kg/day Route of Administration: oral administration (po) 14 days Experimental Results: Inhibited BACE-1, Aβ, APP/Aβ, and tau protein and protected brain tissue in different brain regions. |
References |
[1]. Waiker DK, et al. Design, Synthesis, and Biological Evaluation of Piperazine and N-Benzylpiperidine Hybrids of 5-Phenyl-1,3,4-oxadiazol-2-thiol as Potential Multitargeted Ligands for Alzheimer's Disease Therapy. ACS Chem Neurosci. 2023 Jun 7;14(11):2217-2242.
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Molecular Formula |
C23H23N5O2S
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Molecular Weight |
433.53
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Appearance |
Typically exists as solids (or liquids in special cases) 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 | 2.3066 mL | 11.5332 mL | 23.0665 mL | |
5 mM | 0.4613 mL | 2.3066 mL | 4.6133 mL | |
10 mM | 0.2307 mL | 1.1533 mL | 2.3066 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.