| ln Vitro |
BuChE-IN-23 (compound E14) (20 μM; 24 h) showed very low cytotoxicity against BV2 microglia[1]. BuChE-IN-23 (15 μM; 25 h) effectively inhibited lipopolysaccharide-induced nitric oxide production in BV2 microglia, with an IC50 of 9.76 μM[1].
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| ln Vivo |
BuChE-IN-23 (compound E14) (3-10 mg/kg; orally; once daily; for 14 days) significantly improved recognition, memory and spatial learning abilities in male C57BL/6J mice with oligomer Aβ-induced cognitive impairment and inhibited oAβ-induced hippocampal glial cell activation and neuroinflammation [1]. BuChE-IN-23 (500 mg/kg; orally; single dose) showed good acute tolerability in mice, and no significant organ toxicity was observed after a single oral dose of 500 mg/kg [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types:Mouse microglia BV2 cells Tested Concentrations: 20 μM Incubation Duration: 24 hours Experimental Results: At a concentration of 20 μM, cell viability was maintained above 90%, indicating acceptable cell compatibility. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 3 months old, intraventricular injection of oligomer Aβ1-42 on days 1 and 7) [1]
Doses: 3 mg/kg; 10 mg/kg Route of Administration: Oral; once daily; 14 days Experimental Results: The discrimination ratio was significantly improved compared with the oAβ group, comparable to that of Livasmin. The number of platform crossings was significantly increased compared with the oAβ group, comparable to that of Livasmin. The fluorescence intensity of IBA1 and 6E10 in the hippocampus was significantly reduced, and microglia activation and Aβ deposition were reduced. Compared with the oAβ group, the protein levels of IBA1, GFAP, TLR4 and IL-1β in the hippocampus were significantly downregulated, and the p-p38/p38 ratio was reduced. The fluorescence intensity of GFAP and TNF-α in the hippocampus was significantly reduced, inhibiting astrocyte activation and the expression of pro-inflammatory cytokines. The fluorescence intensity of IL-1β and C3 in the hippocampus was significantly reduced, weakening IL-1β production in microglia and C3 activation in astrocytes. |
| References |
| CAS # |
3067571-93-8
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|---|---|
| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| 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
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| 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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