| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SJ-300 (0-5 μM) significantly reduced DKK3-mLRPIV interaction in SH-SY5Y cells [1]. SJ-300 (1 μM, 2 h) restored Aβ internalization in AD-NSC cells [1]. SJ-300 (10 μM) had no direct effect on the canonical Wnt/β-catenin signaling pathway in SH-SY5Y cells [1]. SJ-300 (50 μM, in 2 μL, 0-60 min) exhibited excellent metabolic stability in mouse and human liver microsomes [1].
|
|---|---|
| ln Vivo |
SJ-300 (single intravenous injection of 2 mg/kg, single intravenous injection of 10 mg/kg) showed stable intravenous concentrations throughout the observation period in C57 mice[1]. SJ-300 (gavage study, 10 mg/kg, single dose) showed brain penetration with a brain/vascular concentration ratio (B/P ratio) of 5732%[1]. SJ-300 (single intravenous injection of 10 mg/kg) showed extremely strong blood-brain barrier activity in C57 mice, with a brain/attention concentration ratio as high as 5732%[1]. SJ-300 (face, 5 mg/kg, once daily for 8 weeks) reconstructed cognitive function in 5×FAD profile AD model mice, and these improvements were associated with Aβ pathology[1]. SJ-300 (face, 5 mg/kg, once daily for 8 weeks) attenuated cognitive deficit AD pathology in 6-month-old 5×FAD mice by enhancing Aβ age[1].
|
| Cell Assay |
Immunofluorescence[1]
Cell Types: AD-NSC cell Tested Concentrations: 1 μM Incubation Duration: 2 h Experimental Results: Restored Aβ internalization in cells treated with DKK3 but in treated with DKK1. |
| Animal Protocol |
Animal/Disease Models: 5×FAD transgenic mouse model of AD (16 weeks)[1]
Doses: 5 mg/kg Route of Administration: i.g., once daily for 8 weeks Experimental Results: Reduced escape latencies during the 5-day acquisition phase. Increased time spent in the target quadrant, and number of platform crossings during the probe trials. Enhanced spatial working memory in the Y-maze test. Reduced the number of Aβ plaques of various diameters in both brain regions. Decreased the total number of Aβ plaques by approximately 73.3%. Decreased the clustering of astrocytes by 64.1 % and microglia around the plaques. Reduced both soluble and insoluble Aβ levels. Did not affect APP cleavage or Aβ production. Animal/Disease Models: 5×FAD transgenic mouse model of AD (6 months)[1] Doses: 5 mg/kg Route of Administration: i.g., once daily for 8 weeks Experimental Results: Did not alter LRP1 expression but reduced colocalized Aβ on brain vascular basement membranes and endothelium. Reduced the levels of both Aβ40 and Aβ42 in the plasma and liver of treated mice. Did not alter the circulating concentrations of soluble LRP1. Inhibited the association between soluble LRP1 (sLRP1) and DKK3. |
| References |
| Molecular Formula |
C20H27FN4
|
|---|---|
| Molecular Weight |
342.45
|
| CAS # |
1210357-06-4
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 | 2.9201 mL | 14.6007 mL | 29.2013 mL | |
| 5 mM | 0.5840 mL | 2.9201 mL | 5.8403 mL | |
| 10 mM | 0.2920 mL | 1.4601 mL | 2.9201 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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