CXCR4 antagonist 4
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2761009-30-5
- Formule: C29H41F2N5
- Masse moléculaire:497.67
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
|
CXCR4 24 nM (IC50) |
HIV 7 nM (IC50) |
In Vitro
CXCR4 antagonist 4 (Compound 30, 0.1~10 µM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:TZM-bl cells
-
Concentration:0.1, 1, 10 µM
-
Incubation Time:48 hours
-
Result:Displayed inhibition potencies against the X4 virus (IC50=7 nM)
In Vivo
| Route | Dose(mg/kg) | T1/2(h) | Cmax(ng/mL) | C12h (ng/mL) | AUC0-8h(h*ng/mL) | % FPO (0-8 h) | Cl (L/h/kg) | Vd (L/kg) |
| iv | 3 | 5.89 | 116 | 265 | 11.3 | 96.3 | ||
| po | 3 | 12.8 | 1.50 | 34.3 | 12.9 | |||
| po | 10 | 54.8 | 14.3 | 190 | 215 | |||
| po | 30 | 169 | 34.8 | 717 | 27.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:mice[1]
-
Dosage:3, 10, 30 mg/kg
-
Administration:
-
Result:Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.
Chemical Information
-
CAS No. 2761009-30-5
-
Masse moléculaire 497.67
-
Formule C29H41F2N5
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CXCR4 antagonist 4 Related Classifications
HY-144285 Related Classifications
Powered by Bioz