| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC50: 0.25 μM (hAChE); 0.23 μM (eeAChE); eqBChE (0.72 μM); 24.12 μM (in DPPH assay)[1]
|
|---|---|
| ln Vitro |
AChE, BChE, and Aβ1-42 can all be efficiently inhibited by AChE-IN-29(VA10)[1]. Cholinesterase inhibitory activity of AChE-IN-29 is demonstrated against hAChE, eeAChE, and eqBChE, with IC50 values of 0.25 μM, 0.23 μM, and 0.72 μM, respectively [1]. Using an IC50 value of 24.12 μM in the DPPH test, AChE-IN-29 demonstrates strong antioxidant activity[1]. Both hAChE- and self-induced Aβ1-42 aggregation can be inhibited by AChE-IN-29 (5 μM, 10 μM, and 20 μM) [1].
|
| ln Vivo |
AChE-IN-29 (VA10), which inhibits AChE activity, improves memory and cognitive impairment (po; 2.5, 5, and 10 mg/kg) [1]. In the hippocampus, AChE-IN-29 (po; 10 mg/kg) increases cell density [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y cells Tested Concentrations: 5, 10, and 20 μM Incubation Duration: 72 h Experimental Results: decreased the Aβ1-42 aggregation and demonstrated no toxic effects on tested cell line(SH-SY5Y). |
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (200 ± 15 g)[1]
Doses: 2.5, 5, and 10 mg/kg Route of Administration: po; one time/day for seven days Experimental Results: Improved cognition and memory in the scopolamine-induced cholinergic deficit. Restores the neuronal cells and can inhibit neuronal toxicity in AD conditions. |
| References |
[1]. Bhanukiran K,et al. Discovery of multi-target directed 3-OH pyrrolidine derivatives through a semisynthetic approach from alkaloid vasicine for the treatment of Alzheimer's disease. Eur J Med Chem. 2023;249:115145.
|
| Molecular Formula |
C18H19BRN2O2
|
|---|---|
| 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.) |
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.
Products are for research use only; We do not sell to patients
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