| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
17β-HSD10-IN-4 (compound 14) (24 hours) effectively inhibited the activity of 17β-HSD10 in HEK-293 cells transfected with pCMV-Neo_17β-HSD10, with an IC50 value of 6.33 ± 0.15 μM[1]. 17β-HSD10-IN-4 (10 hours) showed good blood-brain barrier permeability, with a Pe value of 4.75 ± 0.31 × 10-6 cm·s-1, indicating that it can penetrate into the central nervous system[1].
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|---|---|
| ln Vivo |
17β-HSD10-IN-4 (compound 14) (10 mg/kg; intraperitoneal injection; daily; 14 days) significantly improved cognitive function, restored mitochondrial function, reduced Tau hyperphosphorylation, increased BDNF levels, and reduced Aβ plaque burden in APP/PS1 transgenic mice without altering 17β-HSD10 protein levels [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6 (B6) APPswe/PSEN1dE9 (APP/PS1) transgenic mice (male, 6 months old) [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection; once daily for 14 days Experimental Results: Spatial learning and memory abilities were improved in the treatment group mice. In the Morris water maze probe test, the treatment group mice stayed in the target quadrant for 29 seconds, showing a shortened escape latency, an increased number of platform crossings, and improved target-oriented swimming trajectories. The level of reactive oxygen species (ROS) in the brain cells of APP/PS1 mice decreased by 24%, and the ATP content increased by 76%; cytochrome c release was inhibited to near wild-type levels. Cortical phosphorylated Tau protein (p-Tau) levels decreased by 32%, and the cortical p-Tau/Tau ratio decreased by 18%; hippocampal p-Tau levels decreased by 18%, and the hippocampal p-Tau/Tau ratio decreased by 11%; CDK5 overexpression in the cortex and hippocampus decreased by 13% and 7%, respectively. Compared with untreated APP/PS1 mice, cortical brain-derived neurotrophic factor (BDNF) levels increased by 58%, recovering to near-wild-type levels. Brain Aβ plaque burden was reduced by approximately two-thirds (plaque burden was one-third that of untreated APP/PS1 mice). 17β-HSD10 protein expression showed no significant change compared with untreated APP/PS1 mice. |
| References |
| Molecular Formula |
C14H12N2O3S
|
|---|---|
| Molecular Weight |
288.32
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1C2=C(C(C3=C1N=C(S3)NCCCO)=O)C=CC=C2
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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 | 3.4684 mL | 17.3418 mL | 34.6837 mL | |
| 5 mM | 0.6937 mL | 3.4684 mL | 6.9367 mL | |
| 10 mM | 0.3468 mL | 1.7342 mL | 3.4684 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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