| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Tau Protein Phosphorylation-IN-1 (compound B1) (24 hours) was non-toxic to PC12 cells at a concentration of 30 μM, and significantly resisted Aβ25-35-induced cytotoxicity at a concentration of 10 μM [1]. Tau Protein Phosphorylation-IN-1 (2.5-10 μM, 24 hours) exhibited neuroprotective effects in Aβ25-35-induced PC12 cells through multiple mechanisms, including significantly reducing tau phosphorylation levels at Thr181, Thr205 and Ser396 sites, inhibiting phosphorylation of MAPKs (p38, ERK, JNK) and NF-κB, reversing Aβ-induced upregulation of iNOS and COX-2 expression, regulating the expression of apoptosis-related proteins Bax/Bcl-2 and inhibiting RAGE [1].
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|---|---|
| ln Vivo |
Tau protein phosphorylation-IN-1 (2.5, 5 and 10 mg/kg, intraperitoneal injection, once daily for 28 days) improved cognitive deficits in an Alzheimer's disease model, reduced tau protein hyperphosphorylation, and inhibited neuromodulatory factors [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: PC12 cells Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 24 h Experimental Results: Decreased phosphorylated tau levels at Thr181, Thr205, and Ser396 sites caused by Aβ25–35 compared to the model group. Exhibited stronger inhibition of tau phosphorylation at the Thr181, Thr205, and Ser396 sites than Oleanolic acid (OA) or Donepezil at 10 μM. Reversed the Aβ25–35-induced upregulation of iNOS and COX-2 levels. Significantly inhibited RAGE expression at 5 and 10 μM. Decreased Bax and Bcl-2 expression compared to the control group. Inhibited the phosphorylation of p38 MAPK, ERK and JNK, thereby blocking the MAPK signaling pathway. Reduced the expression of p-NF-κB in Aβ25–35-induced PC12 cells. |
| Animal Protocol |
Animal/Disease Models: Male ICR mice (20-22 g) intracerebroventricularly injected with Aβ₂₅–₃₅ solution (9 nmol/3 μL/mouse) [1]
Doses: 2.5, 5 and 10 mg/kg Route of Administration: i.p., daily for 28 days Experimental Results: Reduced the escape latencies on training days 2-5 compared with the Aβ group in the Morris water maze test. Increased the number of crossings over the original platform location, in contrast to the significant reduction observed in the Aβ group. Reversed the Aβ-induced histopathological damage, including irregular neuronal distribution and reduced cell numbers in the hippocampal CA1 and CA3 areas. Significantly reduced the levels of tau phosphorylation at Thr205, and Ser396 sites, compared with the Aβ group. Significantly decreased the level of tau phosphorylation at the Thr181 site in the hippocampus, especially in the DG, CA1, and CA3 pyramidal neurons. Suppressed the Aβ25-35-induced upregulation of iNOS, COX-2, RAGE, and the Bax/Bcl-2 ratio. Showed an inhibitory effect on p38 MAPK, ERK, and JNK phosphorylation in Aβ25-35-induced AD mice. Inhibited the Aβ25-35-induced upregulation of NF-κB in a dose-dependent manner. Caused no histopathological damage in the liver or kidneys at any tested dose (up to 10 mg/kg) over 21 days. |
| References |
| Molecular Formula |
C39H56N4O3
|
|---|---|
| Molecular Weight |
628.89
|
| CAS # |
3075165-36-2
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5901 mL | 7.9505 mL | 15.9010 mL | |
| 5 mM | 0.3180 mL | 1.5901 mL | 3.1802 mL | |
| 10 mM | 0.1590 mL | 0.7951 mL | 1.5901 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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