| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SGK1-IN-8 (concentration variable; 1 hour of treatment) effectively inhibited recombinant human SGK1 with an IC50 value of 0.11 μM[1]. SGK1-IN-8 (1 μM; pre-incubated for 1 hour, co-incubated with okadaic acid for 24 hours) was non-toxic to SH-SY5Y cells and significantly protected neurons from okadaic acid-induced toxic damage[1]. SGK1-IN-8 (1 μM) did not change the total TAU level in SH-SY5Y cells, but significantly reduced the phosphorylation level of TAU at Ser396 and Ser214 sites[1]. SGK1-IN-8 (10 μM; 120 minutes of treatment) is a substrate of P-glycoprotein. In MDR1-transfected MDCKII cells, its efflux ratio was 2.90 and could be reversed by the P-glycoprotein inhibitor Zosuquidar[1]. SGK1-IN-8 (concentration variable; 30 min) showed weak inhibitory effect on recombinant human GSK3β, with an IC50 of 3.39 μM[1].
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|---|---|
| ln Vivo |
SGK1-IN-8 (compound 55) (5-10 mg/kg; intraperitoneal injection, oral administration; single dose) was rapidly absorbed in male BALB/c mice after a single intraperitoneal or oral administration, resulting in low brain permeability and a brain Kp (AUClast) of 0.04 in both routes [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: SH-SY5Y human neuroblastoma cells (Okada acid-induced AD model) Tested Concentrations: 1 μM (compound 55) Incubation Duration: Pre-incubation for 1 hour; co-incubation with OA for 24 hours Experimental Results: No significant decrease in cell viability was observed at the 1 μM concentration, and the viability of OA-treated SH-SY5Y cells was statistically significantly restored, indicating that it has neuroprotective activity. |
| References |
| Molecular Formula |
C18H13CLN4O
|
|---|---|
| Molecular Weight |
336.78
|
| CAS # |
3109982-48-8
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CNC=C1C2=CC=C(Cl)C=C2)NC3=CC4=C(NN=C4)C=C3
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 2.9693 mL | 14.8465 mL | 29.6930 mL | |
| 5 mM | 0.5939 mL | 2.9693 mL | 5.9386 mL | |
| 10 mM | 0.2969 mL | 1.4846 mL | 2.9693 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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