| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AChE/MAO-B-IN-9 (12 min) effectively inhibited electric eel AChE with an IC50 value of 0.156 ± 0.11 μM, and its selectivity for AChE was 36.79 times higher than that for BuChE [1]. AChE/MAO-B-IN-9 (1 μM; 60 min) inhibited the activity of MAO-B in mouse liver mitochondria by 54.9 ± 2.7% [1]. AChE/MAO-B-IN-9 (0.625-10 μM; up to 80 hours) inhibited the formation of Aβ40 fibers in a concentration-dependent manner with an IC50 value of 10.00 μM [1]. AChE/MAO-B-IN-9 (0.625-10 μM; up to 80 hours) strongly inhibited the formation of Aβ42 fibers in a concentration-dependent manner with an IC50 of 1.01 μM [1]. AChE/MAO-B-IN-9 (2.5-10 μM; treatment time up to 50 hours) inhibited Tau protein fibrosis with an IC50 of 4.50 μM and reduced the fluorescence intensity during the plateau phase by 49% at a concentration of 10 μM [1]. AChE/MAO-B-IN-9 (1.25-20 μM; treatment time 24 hours) inhibited the secretion of Aβ in SH-SY5Y cells in a concentration-dependent manner, and the inhibition rate of total Aβ reached about 80% after treatment at a concentration of 20 μM for 24 hours [1].
|
|---|---|
| ln Vivo |
AChE/MAO-B-IN-9 (1–5 mg/kg; orally; daily; 7 days) dose-dependently improved scopolamine-induced spatial memory deficits in male ICR mice [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: SH-SY5Y cells Tested Concentrations: 10-20 μM Incubation Duration: 24 hours Experimental Results: When used alone, cell viability remained within the normal range (94-97%). Significantly antagonized the toxicity induced by Aβ40 and Aβ42 oligomers, restoring cell survival to control levels. |
| Animal Protocol |
Animal/Disease Models:ICR mice (male, 8 weeks old, SPF grade) [1]
Doses: 1 mg/kg; 5 mg/kg Route of Administration: Oral; once daily for 7 consecutive days Experimental Results: Stable body weight with minimal fluctuations from baseline. In the Morris water maze test, the 1 mg/kg dose group had an average of 3.1 platform crossings. The 5 mg/kg dose group had an average of 3.9 platform crossings. The 5 mg/kg dose group showed highly directional and efficient movement toward the target quadrant on day 5. No pathological changes were observed in the heart, liver, spleen, lungs, and kidneys. |
| References |
| Molecular Formula |
C21H20FN3O3
|
|---|---|
| Molecular Weight |
381.40
|
| CAS # |
2341935-88-2
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC(C2=C(O1)C=CC(F)=C2)=O)NC3=CC=C(N4CCN(C)CC4)C=C3
|
| 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 | 2.6219 mL | 13.1096 mL | 26.2192 mL | |
| 5 mM | 0.5244 mL | 2.6219 mL | 5.2438 mL | |
| 10 mM | 0.2622 mL | 1.3110 mL | 2.6219 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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