| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
E09241 (24 hours) upregulated the OPG/RANKL ratio in stably transfected U-2OS cells, with an EC50 of 1.23 μM [1]. E09241 (0.01-10 μM; 24 hours) upregulated the levels of OPG mRNA, secreted protein, and total protein in MC3T3-E1 cells, and downregulated the levels of RANKL mRNA and secreted protein [1]. E09241 (0.01-10 μM; 12-21 days) promoted osteogenic differentiation of MC3T3-E1 cells, as evidenced by increased ALP activity, mineralization levels, and expression of osteogenic-related genes (Runx2, ALP, Bglap) [1]. E09241 (0.01-10 μM; 1-3 days) inhibited RANKL-induced osteoclast differentiation in RAW264.7 cells by increasing OPG levels, decreasing RANK levels, and downregulating the protein expression of NFATc1 and MMP-9 [1]. E09241 (0.01-10 μM; 24-48 hours) activated the classical Wnt/β-catenin signaling pathway in MC3T3-E1 and C3H10T1/2 cells by increasing β-catenin levels, decreasing DKK1 levels, and enhancing TCF/LEF reporter gene activity [1].
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|---|---|
| ln Vivo |
E09241 (5–20 mg/kg; gavage; daily; 12 weeks) dose-dependently alleviated ovariectomized osteoporosis in rats by increasing bone formation and inhibiting bone resorption, with significant improvements in bone mineral density, relative bone volume and trabecular thickness observed at doses of 5 and 20 mg/kg/day [1].
|
| Animal Protocol |
Animal/Disease Models:Sprague-Dawley rats (7-month-old females, weighing 290-310 g, bilateral ovariectomy + intramuscular dexamethasone, twice a week for 4 weeks)[1]
Doses: 5 mg/kg/day; 20 mg/kg/day Route of Administration: Gavage; once daily for 12 weeks Experimental Results: Reduced trabecular bone loss in a dose-dependent manner. Increased bone mineral density, relative bone volume and trabecular thickness in a dose-dependent manner. Decreased bone surface area/bone volume ratio in a dose-dependent manner. Had no significant effect on trabecular spacing and trabecular number. Femoral structure was improved compared with untreated ovariectomized rats. Reduced the number of osteoclasts per unit bone surface in a dose-dependent manner. At a dose of 20 mg/kg/day, the number of osteoblasts on the bone surface was significantly increased. Osteoporosis levels and the OPG/RANKL ratio increased in a dose-dependent manner. CTX-1 levels, a marker of bone resorption, decreased in a dose-dependent manner. Alkaline phosphatase levels, a marker of bone formation, increased in a dose-dependent manner. |
| References |
| Molecular Formula |
C11H9CLN2O2
|
|---|---|
| Molecular Weight |
236.66
|
| CAS # |
1043110-13-9
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC1=NC=CC(=C1)C)C=2OC(Cl)=CC2
|
| 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
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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 | 4.2255 mL | 21.1274 mL | 42.2547 mL | |
| 5 mM | 0.8451 mL | 4.2255 mL | 8.4509 mL | |
| 10 mM | 0.4225 mL | 2.1127 mL | 4.2255 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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