| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Multi-target AD-IN-7 (compound 3c) showed excellent selectivity for GSK-3β/α in a screening group containing 24 kinases, with an IC50 value of 0.83 nM for GSK-3α and 928 nM for CDK5/p35[1]. Multi-target AD-IN-7 (1-10 μM; 2.5 h) upregulated the level of p-GSK-3β-Ser9 in SH-SY5Y cells, thereby inactivating GSK-3β and upregulating the level of β-catenin in SH-SY5Y cells[1]. Multi-target AD-IN-7 (1-10 μM; pre-incubated for 1 h before 6 h of Aβ25-35 stimulation) inhibited Aβ25-35-induced tau-Ser396 phosphorylation in SH-SY5Y cells in a concentration-dependent manner in vitro[1]. Multi-target AD-IN-7 (10 μM; 24 h) upregulated the mRNA expression levels of neurogenesis-related biomarkers GAP-43 and MAP-2 in SH-SY5Y cells [1]. Multi-target AD-IN-7 (1 μM; 72 h) promoted axonal growth in SH-SY5Y cells, increasing the proportion of cells with axons to 44.11% [1]. Multi-target AD-IN-7 (20 μM mixed with 40 μM metal ions; incubated at room temperature for 30 min) strongly chelated with Alzheimer's disease (AD)-related metal ions Fe2+, Zn2+, Cu2+ and Al3+ (but did not chelate Na+, K+, Mg2+ or Ca2+) [1]. Multi-target AD-IN-7 (20 μM, mixed with 20 μM Aβ1-42; incubated at 37 °C for 24 hours) can inhibit the self-aggregation of Aβ1-42 with an inhibition rate of 33.35%, and can depolymerize the formed Aβ1-42 aggregates by 46.48%. The above results were obtained by ThT fluorescence measurement and transmission electron microscopy (TEM) [1]. Multi-target AD-IN-7 (20 μM, mixed with 20 μM Aβ1-42 and 20 μM Cu2+; incubated at 37 °C for 24 hours) can inhibit Cu2+-mediated Aβ1-42 aggregation with an inhibition rate of 52.18%, and can depolymerize the formed Cu2+-Aβ1-42 aggregates by 56.12%. The above results were obtained by ThT fluorescence measurement [1]. Multi-target AD-IN-7 showed an IC50 of 7.04 μM for scavenging ABTS•+ [1].
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| ln Vivo |
Multitarget AD-IN-7 (1.95–7.81 μM; water exposure; 24 hours) enhanced AlCl3-induced locomotor ability in zebrafish with Alzheimer's disease in a dose-dependent manner [1]. Multitarget AD-IN-7 (1000 mg/kg; oral; single dose) showed low acute toxicity in C57BL/6 mice. No death, behavioral abnormalities, weight changes, or organ pathological changes were observed within 14 days after a single oral dose of 1000 mg/kg [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: SH-SY5Y cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 2.5 hours Experimental Results: p-GSK-3β-Ser9 levels increased in a concentration-dependent manner, with p-GSK-3β-Ser9/GAPDH ratios of 0.43, 0.63, and 0.76 at concentrations of 1, 5, and 10 μM, respectively. β-catenin levels increased in a concentration-dependent manner, with β-catenin/GAPDH ratios of 0.32, 0.39, and 0.51 at concentrations of 1, 5, and 10 μM, respectively. Western Blot Analysis [1] Cell Types: SH-SY5Y cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 1 hour (pre-incubated before 6-hour Aβ25-35 stimulation) Experimental Results: p-tau-Ser396 levels decreased in a concentration-dependent manner. The p-tau-Ser396/GAPDH ratios at 1, 5, and 10 μM were 0.31, 0.24, and 0.18, respectively. RT-PCR[1] Cell Types: SH-SY5Y cells Tested Concentrations: 10 μM Incubation Duration: 24 hours Experimental Results: The mRNA expression of GAP-43 and MAP-2 was upregulated to a level higher than that of the positive control retinoic acid. |
| Animal Protocol |
Animal/Disease Models:Wild-type AB (juvenile fish, 4 days post-fertilization) [1]
Doses: 1.95 μM; 3.91 μM; 7.81 μM Route of Administration: Water exposure; 24 hours Experimental Results: At a concentration of 1.95 μM, AlCl3 induced an increase in swimming distance of 1314 mm in AD zebrafish. At a concentration of 3.91 μM, AlCl3 induced an increase in swimming distance of 1716 mm in AD zebrafish. At a concentration of 7.81 μM, AlCl3 induced an increase in swimming distance of 2040 mm in AD zebrafish, while the swimming distance of the control group induced by AlCl3 was 996 mm. Animal/Disease Models:C57BL/6 (6-8 weeks old, male and female) [1] Doses: 1000 mg/kg Route of Administration: Oral; single dose Experimental Results: No death or abnormal behavior was observed within 14 days. There was no significant change in body weight compared to the control group. No significant differences in size or shape were observed in the anatomical organs (heart, liver, spleen, lungs, kidneys, brain). HE staining showed no significant pathological changes in the organs. |
| References |
| Molecular Formula |
C28H19N5O2
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|---|---|
| Molecular Weight |
457.48
|
| CAS # |
3113741-59-3
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
OC1=CC(C2=CN=C(NC=C3C(NC4=C(C5=CC=CC=C5)C=CN=C4)=O)C3=C2)=CC6=C1N=CC=C6
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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 | 2.1859 mL | 10.9294 mL | 21.8589 mL | |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1859 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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