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).
For research use only. We do not sell to patients.
- CAS No.: 2761009-30-5
- Formula: C29H41F2N5
- Molecular Weight:497.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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CXCR4 24 nM (IC50) |
HIV 7 nM (IC50) |
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.
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Cell Line:TZM-bl cells
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Concentration:0.1, 1, 10 µM
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Incubation Time:48 hours
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Result:Displayed inhibition potencies against the X4 virus (IC50=7 nM)
| 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.
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Animal Model:mice[1]
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Dosage:3, 10, 30 mg/kg
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Administration:
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Result:Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.
Chemical Information
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CAS No. 2761009-30-5
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Molecular Weight 497.67
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Formula C29H41F2N5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)