| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BChE-IN-13 (5-100 μM; 24 h) exhibits severe mortality to BV2 cells and mild toxicity to PC-12, HT-22, and SH-SY5Y [1]. Using the Parallel Artificial Membrane Permeability Assay (PAMPA), BChE-IN-13 demonstrated outstanding blood-brain barrier permeability[1].
|
|---|---|
| ln Vivo |
BChE-IN-13 (oral gavage; 15 mg/kg; once daily; 6 days) showed improved memory and cognitive function in mice with Aβ1-42-induced AD-like disease [1].
|
| Cell Assay |
Cytotoxicity assay [1]
Cell Types: SH-SY5Y, PC12, BV2 and HT-22 Cell Tested Concentrations: 5-100 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated cell viability over SH-SY5Y, PC-12 and 60% HT- 22 This is true even at 100 μM. demonstrated high mortality in BV2 cells, reaching half the mortality rate at 20 μM. |
| Animal Protocol |
Animal/Disease Models: ICR mice intracerebroventricular (icv) injection of oligomeric Aβ1-42
Doses: 15 mg/kg Route of Administration: po (oral gavage); 15 mg/kg; one time/day; 6 days Experimental Results: Compared with donepezil, memory and Cognitive function is improved and the latency period is shorter. |
| References |
[1]. Xin Lu, et al. Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.
|
| Exact Mass |
360.22
|
|---|---|
| CAS # |
2700896-73-5
|
| PubChem CID |
156786229
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
463
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC=CC=C1NC(=O)CN(CC2=CC3=CC=CC=C3C=C2)CC(C)C
|
| InChi Key |
ULIOAMNTKXKLNZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H28N2O/c1-18(2)15-26(17-24(27)25-23-11-7-4-8-19(23)3)16-20-12-13-21-9-5-6-10-22(21)14-20/h4-14,18H,15-17H2,1-3H3,(H,25,27)
|
| Chemical Name |
N-(2-methylphenyl)-2-[2-methylpropyl(naphthalen-2-ylmethyl)amino]acetamide
|
| 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.) |
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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