2. Stem Cell/Wnt Immunology/Inflammation Metabolic Enzyme/Protease NF-κB
  3. Wnt β-catenin Nuclear Factor of activated T Cells (NFAT) MMP RANKL/RANK
  4. 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.

For research use only. We do not sell to patients.

E09241

E09241 Chemical Structure

CAS No. : 1043110-13-9

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E09241 Related Antibodies

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Description

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[1].

In Vitro

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.

E09241 Related Antibodies

Cell Differentiation Assay[1]

Cell Line: MC3T3-E1 mouse calvarial preosteoblasts
Concentration: 0.01-10 μM (ALP activity and gene expression; mineralization)
Incubation Time: 12 days (ALP activity and gene expression); 21 days (mineralization)
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.
In Vivo

E09241 (5-20 mg/kg; i.g.; daily; 12 weeks) dose-dependently attenuates ovariectomy-induced 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (7-month-old female, 290-310 g, bilateral ovariectomy + intramuscular dexamethasone twice weekly for 4 weeks)[1]
Dosage: 5 mg/kg/day; 20 mg/kg/day
Administration: i.g.; daily; 12 weeks
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.
Molecular Weight

236.66

Formula

C11H9ClN2O2
CAS No.
SMILES

O=C(NC1=NC=CC(=C1)C)C=2OC(Cl)=CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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E09241 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E092411043110-13-9E 09241E-09241Wntβ-cateninNuclear Factor of activated T Cells (NFAT)MMPRANKL/RANKBeta cateninMatrix metalloproteinasesosteoclast differentiationNFATc1osteoprotegerinosteogenic differentiationMMP-9U-2OS cellscanonical Wnt/β-catenin signalingDKK1RANKLInhibitorinhibitorinhibit

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