| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CGK012 (0-20 μM) inhibits HMGB1 release by inhibiting LPS-induced HMGB1 acetylation and SIRT1 expression, thereby reducing excessive vascular permeability in HUVECs and reducing the expression of pathogen-related molecules such as TLR2/4 without affecting HUVEC cell viability[1]. CGK012 (0-20 μM) improves inflammatory responses by reducing the adhesion and migration of inflammatory immune cells and inhibiting the production of proinflammatory cytokines such as IL-6, TNF-α, β, and transcription factors NF-kB and ERK1/2[1]. CGK012 (0-20 μM) promotes β-catenin phosphorylation and degradation and inhibits the expression of β-catenin-dependent genes, inhibiting the proliferation of multiple myeloma cells RPMI-8226 with an IC50 of 5.08 μM[2].
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|---|---|
| ln Vivo |
CGK012 (0.05-0.53 mg/kg, intravenous injection, double dose) inhibits HMGB1 release and immune cell migration, and improves vascular cell stability and mouse survival in C57BL/6 mice induced by sepsis by cecal ligation and puncture[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HUVEC Concentration: 5-100 μM Incubation Duration: 48 h Experimental Results: Revealed no effects on cell viability. Western Blot Analysis[1] Cell Types: HUVECs, HEK293-FL reporter, RPMI-8226 Concentration: 0-20 μM Incubation Duration: 12 h Experimental Results: Reduced levels of SIRT1 and acetylation of HMGB1, inhibited vascular permeability in HUVECs. Reduced levels of β-catenin in HEK293-FL reporter and RPMI-8226. Cell Migration Assay [1] Cell Types: HUVEC Concentration: 0-20 μM Incubation Duration: 6 h Experimental Results: Inhibited migration of neutrophils through monolayers of HUVECs. |
| Animal Protocol |
Animal/Disease Models:CLP- induced sepsis in C57BL/6 mice[1]
Doses: 0.26-0.53 mg/kg Route of Administration: double doses, 12 or 50 h after surgery. Experimental Results: Reduced expression of HMGB1 and improved the survival rate. |
| References |
| Molecular Formula |
C20H23NO5
|
|---|---|
| Molecular Weight |
357.40
|
| CAS # |
2044497-76-7
|
| Appearance |
Typically exists as solid 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 | 2.7980 mL | 13.9899 mL | 27.9799 mL | |
| 5 mM | 0.5596 mL | 2.7980 mL | 5.5960 mL | |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7980 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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