| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MAO-B-IN-45 (compound 21d) is a reversible hMAO-B inhibitor with an inhibition constant Ki of 100.6 nM, exhibiting high hMAO-B inhibitory activity with inhibition rates of 94.81% (10 μM) and 76.31% (1 μM) [1]. MAO-B-IN-45 (0.1-75 μM, 24 h) showed good safety in both PC12 and HT22 cells [1]. MAO-B-IN-45 (1-50 μM, 24 h) effectively reduced RSL3 or Erastin-induced ferroptosis in HT22 cells in a dose-dependent manner [1]. MAO-B-IN-45 (10-50 μM, 24 h) reduced intracellular ROS production in HT22 cells [1]. MAO-B-IN-45 (15-100 μM, 24 h) effectively inhibited ferroptosis by reducing intracellular iron accumulation and enhancing the GSH-dependent pathway in HT22 cells [1].
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|---|---|
| ln Vivo |
MAO-B-IN-45 (compound 21d) (10 mg/kg, intraperitoneal injection, once daily for 35 days) can alleviate memory and cognitive dysfunction in a 3×Tg(APP/Tau/Ps1) AD mouse model and has shown good safety in vivo [1].
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| Cell Assay |
Cytotoxicity assay [1] Cell Types: HT22 cells, PC12 cells Test concentrations: 25, 50 and 75 μM (HT22 cells), 0.1, 1, 10, 20, 30, 40, 50 and 75 μM (PC12 cells)
Incubation Duration: 24 hours Experimental Results: The assay showed good safety. At the highest test concentration (75 μM), the cell viability of PC12 cells remained at 83.56% and that of HT22 cells remained at 86.47%, which warrants further investigation. Cytotoxicity assay [1] Cell Types: RSL3/Erastin-induced HT22 cells Tested Concentrations: 1, 5, 10, 25, 50 μM Incubation Duration: 24 hours Experimental Results: At a concentration of 10 μM, RSL3 and Erastin reduced induced ferroptosis and at a concentration of 50 μM, cell viability was fully restored to normal levels. |
| Animal Protocol |
Animal/Disease Models:Triple transgenic (APP/Tau/Ps1) mice (30-35 g, 7 months)[1].
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection daily for 35 days Experimental Results: Increased the number of times the mice entered the platform, shortened the latency period and the distance to reach the platform, with effects comparable to the safinamide group and donepezil group. Cognitive function was not significantly different from wild-type mice. No abnormalities were observed in tissues (heart, liver, spleen, lung, kidney) compared to wild-type mice (H&E staining). FTH1 levels in 3×Tg mice returned to normal, and GPX4 expression levels were significantly increased. APP protein levels were reduced, and the specificity of p-Tau at the Ser202/Thr205 site was reduced. |
| References |
| Molecular Formula |
C17H14CLNO3
|
|---|---|
| Molecular Weight |
315.75
|
| CAS # |
3069915-36-9
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CN1C(C(O)=CC2=CC=C(C=C21)OCC3=CC=C(C=C3)Cl)=O
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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)
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| 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 | 3.1671 mL | 15.8353 mL | 31.6706 mL | |
| 5 mM | 0.6334 mL | 3.1671 mL | 6.3341 mL | |
| 10 mM | 0.3167 mL | 1.5835 mL | 3.1671 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.
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