| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BuChE-IN-20 (compound 4d-13) (5 μM, 10 min) showed selectivity for BuChE by enzyme activity assays of hAChE and hBuChE [1]. BuChE-IN-20 (20 μM, 48 h) prevented the aggregation and deposition of Aβ1-42, thereby exerting neuroprotective effects by inhibiting the formation of toxic amyloid plaques and mitigating Aβ1-42-induced neurotoxicity by reducing ROS production [1]. BuChE-IN-20 (1 mM, 30 min) had a 775-fold greater scavenging capacity for hydroxyl radicals than vitamin C [1]. BuChE-IN-20 (5-10 μM, 4 h pretreatment, 8 h co-treatment with LPS) reduced LPS (1.5 μg/mL)-induced levels of reactive oxygen species (ROS) in RAW264.7 cells in a concentration-dependent manner [1]. BuChE-IN-20 (6.25-12.5 μM, pretreatment for 4 hours, co-treatment with LPS for 24 hours) significantly inhibited NO production in RAW264.7 cells induced by LPS (2 μg/mL) [1]. BuChE-IN-20 (1-100 μM, 24 hours) could inhibit mouse BV-2 cell lines and scavenge free radicals at submicromolar concentrations, with a cytotoxic safety factor close to 150 times [1]. BuChE-IN-20 (1-10 μM, pretreatment for 24 hours, co-treatment with LPS for 24 hours) reduced IL-1β levels in BV-2 cells induced by LPS (100 ng/mL) [1]. BuChE-IN-20 (1-20 μM, pretreated for 6 hours and co-treated with NMDA/L-glutamate for 24 hours) can dose-dependently reduce cytotoxicity in a NMDA (20 mM)/L-glutamate (Glu) (B)-induced SH-SY5Y cell injury model [1].
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|---|---|
| ln Vivo |
BuChE-IN-20 (compound 4d-13) (10-100 mg/kg, orally, single dose) showed no toxicity or abnormal symptoms at the maximum tolerated dose of 100 mg/kg in an ICR mouse model [1]. BuChE-IN-20 (10-40 mg/kg, orally, single dose) significantly improved learning and memory function in ICR mice induced by scopolamine hydrobromide (3 mg/kg, intraperitoneal injection) [1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: LPS (100 ng/mL) induced BV-2 cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 24-hour pretreatment and 24-hour co-treatment with LPS Experimental Results: IL-1β expression decreased in a dose-dependent manner, while the effect on IL-6 and TNF-α was relatively small. It directly inhibited the production, release, and NLRP3-mediated maturation of IL-1β. It indirectly reduced IL-1β expression by inhibiting the NF-κB and MAPK signaling pathways. |
| Animal Protocol |
Animal/Disease Models:ICR mice induced by scopolamine hydrobromide (3 mg/kg, intraperitoneal injection)[1]
Doses: 10-40 mg/kg< Route of Administration: Gavage (po) Experimental Results: The hippocampal-dependent memory and spatial learning impairments induced by scopolamine hydrobromide were restored. Gavage administration of 40 mg/kg of scopolamine hydrobromide alleviated the cognitive impairments induced by it, manifested as a shortened escape latency and a reduced distance traveled to the escape platform. |
| References |
| Molecular Formula |
C29H29FN4O2
|
|---|---|
| Molecular Weight |
484.56
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
OC1=C(F)C=C(CN[C@@H](CC2=CNC3=CC=CC=C32)C(N(C)CCC4=CNC5=C4C=CC=C5)=O)C=C1
|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0637 mL | 10.3186 mL | 20.6373 mL | |
| 5 mM | 0.4127 mL | 2.0637 mL | 4.1275 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0637 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.
Products are for research use only; We do not sell to patients
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