| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
17β-HSD10/CDK5-IN-1 (compound 5l) binds to CDK5 and 17β-HSD10 with binding free energies of -9.72 and -9.74 Kcal/mol, respectively[1].
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|---|---|
| ln Vivo |
17β-HSD10/CDK5-IN-1 (compound 5l) (10 mg/kg; intraperitoneal injection; daily; 14 days) significantly improved cognitive function, reduced oxidative stress, restored mitochondrial function, alleviated Tau pathology, enhanced neurotrophic support, reduced Aβ deposition, and inhibited neuroinflammation in a mouse model of Alzheimer's disease [1].
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| Animal Protocol |
Animal/Disease Models: Male APP/PS1 mice (6 months old) and wild-type C57BL/6 mice [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection; once daily for 14 days Experimental Results: In the Morris water maze training, the escape latency of mice was shortened, the time spent in the target quadrant was increased, and the number of times they crossed the platform in the probe test was increased. The level of reactive oxygen species (ROS) in the brain of APP/PS1 mice was reduced by 41%. The level of adenosine triphosphate (ATP) in the brain of APP/PS1 mice was increased by 86%. The level of cytochrome c in the cortex was reduced by 20%, and the level of cytochrome c in the hippocampus was reduced by 15%, returning to near the level of wild type. Compared with the APP/PS1 model group, the expression of 17β-HSD10 protein in the cortex or hippocampus was not significantly changed. Compared to the APP/PS1 model group, hippocampal CDK5 expression decreased by 22%; cortical CDK5 expression showed no significant change. Hippocampal p-Tau levels and the p-Tau/Tau ratio were decreased. Cortical BDNF content increased by 76% compared to the APP/PS1 model group, reaching levels comparable to wild-type mice. Aβ plaque burden in APP/PS1 mice was reduced to approximately one-third of that in the model group. The activated area of IBA1-positive microglia was reduced to approximately one-quarter of that in the APP/PS1 model group, approaching the level of the positive control group. |
| References |
| Molecular Formula |
C21H25N3O4
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|---|---|
| Molecular Weight |
383.44
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=C2C=CC=C1)C3=C(C(NC(NCCCN(CC)CC)=O)=C(C)O3)C2=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 | 2.6080 mL | 13.0398 mL | 26.0797 mL | |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 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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