Physicochemical Properties
| Molecular Formula | C30H26F3NO3 |
| Molecular Weight | 505.53 |
| 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) |
Biological Activity
| Targets | MAO-B 0.41 ± 0.0 μM (IC50) EeAChE 0.58 ± 0.0 μM (IC50) |
| ln Vitro | Compound C10, dual AChE-MAO B-IN-3, has minimal neurotoxicity (0–100 μM, 24 hours) and powerfully suppresses AChE enzymatic activity (0–10 μM, 24 hours)[1]. In SH-SY5Y cells, dual AChE-MAO B -IN-3 considerably lessens glutaraldehyde-induced tau protein phosphorylation and strongly suppresses AChE-induced amyloid aggregation, protecting against mitochondrial dysfunction and oxidation more efficiently than donepezil[1]. |
| ln Vivo | In a scopolamine-induced AD mice model, dual AChE-MAO B-IN-3 (compound C10) (10 mg/kg, IP, once daily for 10 consecutive days) exhibits significantly improved improvements in cognitive activities and spatial memory with more efficacy than donepezil (HY-14566)[1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: SH-SY5Y cells Tested Concentrations: 10 μM, 50 μM, 100 μM Incubation Duration: 24 h Experimental Results: demonstrated a nonsignificant reduction in cell viabilities up to the maximum tested concentration of 100 μM. The percentage cell viability at 10-100 μM was observed in the range of 96.92−99.58%. demonstrated that compound C10 was not toxic to SH-SY5Y neuroblastoma cells at concentrations up to 100 μM. |
| Animal Protocol |
Animal/Disease Models: ICR mice (female, 8-10 weeks, 25-30 g)[1] Doses: 10 mg/kg Route of Administration: IP, one time/day for 10 days Experimental Results: Dramatically ameliorated the cognitive impairment in a scopolamine-induced mice model. |
| References |
[1]. Design, Synthesis, and Biological Evaluation of Novel Chromanone Derivatives as Multifunctional Agents for the Treatment of Alzheimer's Disease. ACS Chem Neurosci. 2022 Nov 16. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9781 mL | 9.8906 mL | 19.7812 mL | |
| 5 mM | 0.3956 mL | 1.9781 mL | 3.9562 mL | |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9781 mL |