E8431 |
Catalog No.GC81443
One-Click Copy Product Info
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E8431 is a DCSTAMP antagonist with an IC50 value of 775.8 nM for osteoclastogenesis.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2419580-01-9
Sample solution is provided at 25 µL, 10mM.
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In Vivo, E8431 (100 mg/kg; i.p.; once daily; 6 weeks) completely reverses ovariectomy-induced osteoporosis in ovariectomized (OVX) mouse models by inhibiting osteoclast maturation, promoting osteoblast activity and angiogenesis, with no obvious toxicity[1].
In Vitro, E8431 (10 nM-10 μM; 5 days) potently inhibits M-CSF/RANKL (/)-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].
References:
[1]. Zhang Z, et al. A novel DCSTAMP antagonist impedes preosteoclast fusion via modulation of RAP1B-RAC1-mediated cytoskeletal remodeling. Experimental & molecular medicine. 2025 Dec;57(12):2898-2915.
| Cas No. | 2419580-01-9 | SDF | |
| Formula | C24H26N2O3 | M.Wt | 390.47 |
| Solubility | DMSO: 30 mg/mL (76.83 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.561 mL | 12.8051 mL | 25.6102 mL |
| 5 mM | 512.2 μL | 2.561 mL | 5.122 mL |
| 10 mM | 256.1 μL | 1.2805 mL | 2.561 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)