| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
hAChE 0.113 μM (IC50) hBACE-1 0.38 μM (IC50) hBCHE 1.48 μM (IC50)
|
|---|---|
| ln Vitro |
In the SH-SY5Y neuroblastoma cell line, the safety profile of hAChE/hBACE-1-IN-2 (compound 5f) (10-80 μM, 72 h) is thought to be comparable to that of donepezil [1]. Compound 5f (hAChE/hBACE-1-IN-2; 20 μM; 48 h, 72 h) has the ability to withstand the aggregation potential of Aβ1-42 in the neuroblastoma cell line SH-SY5Y [1]
|
| ln Vivo |
hAChE/hBACE-1-IN-2 (2.5–10 mg/kg, oral, 14 days) alleviates RTL and splay in a mouse model of arm time cognitive impairments caused by scopolatin (HY-N0296)[1]. In Swiss albino mice, hAChE/hBACE-1-IN-2 (500 mg/kg, oral, 14 days) was well tolerated and showed no signs of toxicity, such as abnormalities in the liver, kidneys, heart, or brain [1]. 10 mg/kg oral hAChE/hBACE-1-IN-2 for 14 days reduces AchE levels in the hippocampus and cortical brain homogenates in a mouse model of Scopolamine (HY-N0296) or substrate hydrolysis, has the ability to postpone oxidative stress, and lowers levels of pro-inflammatory cytokines [1]. It also passes the blood-brain barrier. In Aβ-induced models, hAChE/hBACE-1-IN-2 (10 mg/kg, oral, 14 days) preserves brain tissue in several brain regions by inhibiting the levels of BACE-1, Aβ, APP/Aβ, and tau protein [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y cell lines(The SH-SY5Y cells were sequentially treated with RA and BDNF for 6 days) Tested Concentrations: 10, 20, 40, and 80 μM Incubation Duration: 48-72 h Experimental Results: Indicated a similar reduction in the differentiated neuroblastoma cell population at a maximum 80 μM concentration. Cell Viability Assay[1] Cell Types: Aβ1-42 treated SH-SY5Y cells(incubated with Aβ1-42(10μM) for 24 h) Tested Concentrations: 20 μM Incubation Duration: 48-72 h Experimental Results: The cells incubated the cell viability to 65% and 75% after 48 h and 72 h. |
| Animal Protocol |
Animal/Disease Models: Swiss albino mice[1]
Doses: 500 mg/kg Route of Administration: Oral administration (po), 14 days Experimental Results: demonstrated no signs or symptoms of toxicity over the 14 days Animal/Disease Models: Scopolamine-induced cognitive deficit mouse model[1 ] Doses: 2.5 mg, 5 mg, and 10 mg/kg Route of Administration: Oral administration (po), 14 days Experimental Results: Elevated plus maze test demonstrated significant reductions in transfer latency and time spent in open arms, similar to the effects observed with Scopolamine (HY-N0296)-induced dementia reversal. |
| References |
| Molecular Formula |
C22H24N4O2S
|
|---|---|
| Molecular Weight |
408.52
|
| Appearance |
Typically exists as solid at room temperature
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 2.4479 mL | 12.2393 mL | 24.4786 mL | |
| 5 mM | 0.4896 mL | 2.4479 mL | 4.8957 mL | |
| 10 mM | 0.2448 mL | 1.2239 mL | 2.4479 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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