E8431
Based on 1 Customer Validation
E8431 is a DCSTAMP antagonist with an IC50 value of 775.8 nM for osteoclastogenesis. E8431 selectively binds to the endoplasmic reticulum domain of DCSTAMP, disrupts its interaction with RAP1B, and inhibits downstream cytoskeleton rearrangement mediated by the RAP1-RAC1 signaling pathway, thereby impeding osteoclast precursor fusion, suppressing bone resorption, and stimulating PDGFBB secretion to promote osteogenesis and angiogenesis. E8431 can be used in the research of osteoporosis.
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- Purity: 97.34%
- CAS No.: 2419580-01-9
- 화학식: C24H26N2O3
- 분자량:390.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PI3K |
E8431 (10 nM-10 μM; 5 days) potently inhibits M-CSF/RANKL (HY-P7247/HY-P73388)-induced osteoclastogenesis in primary mBMMs, with an IC50 of 0.7758 μM. It shows no cytotoxicity at concentrations up to 10 μM and binds to human and mouse DCSTAMP with high affinity[1].
E8431 (0.5-2 μM; 5 days) dose-dependently inhibits osteoclastogenic activity and downregulates the mRNA expression levels of osteoclast-specific markers in mouse mBMMs and human PBMCs[1].
E8431 (10 nM-50 μM; 24-48 h) exhibits excellent cytocompatibility in mouse primary bone marrow mononuclear macrophages (mBMMs), mouse endothelial progenitor cells (mEPCs), mouse bone marrow mesenchymal stem cells (mBMSCs), human peripheral blood mononuclear cells (PBMCs), human umbilical vein endothelial cells (HUVECs), and human bone marrow mesenchymal stem cells (hBMSCs), with no significant cytotoxicity at concentrations below 10 μM (mouse cells) or 20 μM (human cells)[1].
E8431 (0.5-2 μM; co-cultured for 4-24 h) exhibits significant activity in promoting endothelial cell migration and vascular tube formation in mEPCs co-cultured with mBMMs and HUVECs co-cultured with PBMCs, by promoting PDGFBB secretion from pre-osteoclasts[1].
E8431 (0.5-2 μM; co-culture induction for 6-14 days) exhibits osteogenic differentiation-promoting activity in mBMSCs co-cultured with mBMMs and hBMSCs co-cultured with PBMCs, significantly increasing ALP activity, OCN expression, and mineralized nodule formation[1].
E8431 (2 μM; co-culture treatment for 5-60 min) significantly activates the phosphorylation of PDGFRβ, PI3K, Akt and FAK in co-cultured mouse mEPCs and mBMSCs[1].
E8431 (2 μM; 5 days) blocks the RAP1-RAC1 signaling pathway and significantly disrupts the interaction between DCSTAMP and RAP1B in mouse mBMMs[1].
E8431 (0.5-2 μM; 5 days) dose-dependently inhibits osteoclastogenic activity and downregulates the mRNA expression levels of osteoclast-specific markers in mouse mBMMs and human PBMCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine mBMMs, mEPCs, mBMSCs; Human PBMCs, HUVECs, hBMSCs
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Concentration:10 nM, 50 nM, 100 nM, 500 nM, 1 μM, 2 μM, 5 μM, 10 μM, 20 μM, 50 μM
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Incubation Time:24 h ; 48 h
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Result:Exhibited no significant cell proliferation toxicity at concentrations up to 10 μM in murine cells.
Maintained excellent cell viability at concentrations up to 20 μM in human cells.
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Cell Line:Murine mBMMs, Human PBMCs, Co-cultured murine/human BMSCs
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:5 days or 14 days
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Result:Significantly downregulated the mRNA expression of Oscar and Ctsk in osteoclasts.
Upregulated the mRNA levels of Runx2, Alp, and Bglap (OCN) in co-cultured BMSCs.
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Cell Line:Murine mEPCs and human HUVECs co-cultured with osteoclast conditioned media
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Concentration:0.5 μM, 2 μM
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Incubation Time:24 h
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Result:Significantly enhanced the migration rate and the number of migrated cells compared to the control, especially at the 2 μM dose.
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Cell Line:Murine mEPCs and human HUVECs co-cultured with osteoclast conditioned media
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Concentration:0.5 μM, 2 μM
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Incubation Time:24 h
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Result:Significantly enhanced the migration rate and the number of migrated cells compared to the control.
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Cell Line:Murine mBMMs, Co-cultured murine mEPCs and mBMSCs
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Concentration:2 μM
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Incubation Time:5 days (mBMMs); 0, 5, 15, 30, 60 minutes (co-cultured cells)
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Result:Decreased the activation levels of RAP1-GTP and RAC1-GTP, and inhibited the phosphorylation of Syk and Src in mBMMs.
Upregulated the expression of p-PDGFRβ, p-PI3K, p-Akt, and p-FAK in co-cultured endothelial and mesenchymal stem cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type mice (ovariectomized, 6-week postsurgical recovery)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 6 weeks
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Result:Restored bone volume fraction (BV/TV), bone mineral density (BMD), trabecular number, and trabecular thickness to sham-operated levels.
Reduced trabecular separation.
Normalized serum bone turnover markers (CTX-1 and PINP).
Reduced TRAP-positive multinucleated mature osteoclasts.
Increased TRAP-positive mononuclear preosteoclasts.
Expanded OCN-positive osteoblast populations.
Restored ovariectomy-suppressed bone formation rate (BFR/BS).
Recovered ovariectomy-reduced CD31hiEMCNhi type H endothelial cell populations in bone marrow.
Elevated bone marrow PDGFBB levels.
Showed no significant changes in serum cardiac, hepatic, or renal injury markers, nor pathological changes in major organs (heart, lung, liver, spleen, kidney).
Chemical Information
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CAS No. 2419580-01-9
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Appearance Solid
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분자량 390.47
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화학식 C24H26N2O3
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(NC(N3CC4(C5=CC=CC=C5CC4)OCC3)=O)=CC=C2CCCC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 30 mg/mL (76.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (287 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5610 mL | 12.8051 mL | 25.6102 mL | 64.0254 mL |
| 5 mM | 0.5122 mL | 2.5610 mL | 5.1220 mL | 12.8051 mL | |
| 10 mM | 0.2561 mL | 1.2805 mL | 2.5610 mL | 6.4025 mL | |
| 15 mM | 0.1707 mL | 0.8537 mL | 1.7073 mL | 4.2684 mL | |
| 20 mM | 0.1281 mL | 0.6403 mL | 1.2805 mL | 3.2013 mL | |
| 25 mM | 0.1024 mL | 0.5122 mL | 1.0244 mL | 2.5610 mL | |
| 30 mM | 0.0854 mL | 0.4268 mL | 0.8537 mL | 2.1342 mL | |
| 40 mM | 0.0640 mL | 0.3201 mL | 0.6403 mL | 1.6006 mL | |
| 50 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2805 mL | |
| 60 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0671 mL |
E8431 Related Classifications
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