E09241
E09241 is an orally active osteoclastogenesis inhibitor. E09241 reduces the RANKL-induced expression of NFATc1 and MMP-9 by activating Wnt/β-catenin. E09241 increases the OPG/RANKL ratio by upregulating OPG expression, inhibits bone resorption, promotes bone formation and prevents ovariectomy-related bone loss. E09241 can be used in the research of osteoporosis.
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- CAS. Nr.: 1043110-13-9
- Formel: C11H9ClN2O2
- Molecular Weight:236.66
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | Inhibition |
32.4 %
Compound: DDD01062615
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Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 10uM
Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 10uM
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[PMID: 32078764] |
| HepG2 | Inhibition |
4.14 %
Compound: DDD01062615
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Toxicity liver stage against HepG2, at 10uM
Toxicity liver stage against HepG2, at 10uM
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[PMID: 32078764] |
| HepG2 | Inhibition |
5.48 %
Compound: DDD01062615
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Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 2uM
Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 2uM
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[PMID: 32078764] |
E09241 (24 h) upregulates the OPG/RANKL ratio in stably transfected U-2OS cells, with an EC50 of 1.23 μM[1].
E09241 (0.01-10 μM; 24 h) upregulates the levels of OPG mRNA, secreted protein and total protein, and downregulates the levels of RANKL mRNA and secreted protein in MC3T3-E1 cells[1].
E09241 (0.01-10 μM; 12-21 days) promotes osteoblastic differentiation in MC3T3-E1 cells, with increased ALP activity, mineralization levels, and the expression of osteogenesis-related genes (Runx2, ALP, Bglap)[1].
E09241 (0.01-10 μM; 1-3 days) inhibits RANKL-induced osteoclast differentiation of 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 h) activates the canonical 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MC3T3-E1 mouse calvarial preosteoblasts
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Concentration:0.01-10 μM (ALP activity and gene expression; mineralization)
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Incubation Time:12 days (ALP activity and gene expression); 21 days (mineralization)
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Result:Significantly increased ALP activity at 1, 10 μM.
Increased mineralized nodule formation at 1, 10 μM.
Increased Runx2 mRNA levels at 1, 10 μM, ALP mRNA levels at 1, 10 μM, and Bglap mRNA levels at 0.1, 1, 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (7-month-old female, 290-310 g, bilateral ovariectomy + intramuscular dexamethasone twice weekly for 4 weeks)[1]
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Dosage:5 mg/kg/day; 20 mg/kg/day
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Administration:i.g.; daily; 12 weeks
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Result: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/bone volume ratio in a dose-dependent manner.
Did not significantly affect trabecular separation and trabecular number.
Improved femur structure compared to untreated ovariectomized rats.
Reduced the number of osteoclasts per bone surface in a dose-dependent manner.
Significantly increased the number of osteoblasts per bone surface at 20 mg/kg/day.
Increased osteoprotegerin levels and the OPG/RANKL ratio in a dose-dependent manner.
Reduced levels of the bone resorption marker CTX-1 in a dose-dependent manner.
Increased levels of the bone formation marker alkaline phosphatase in a dose-dependent manner.
Chemical Information
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CAS. Nr. 1043110-13-9
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Molecular Weight 236.66
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Formel C11H9ClN2O2
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SMILES
O=C(NC1=NC=CC(=C1)C)C=2OC(Cl)=CC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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