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Mavorixafor (AMD-070) is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
In vitro: AMD-070 is confirmed against X4 strain of HIV-1, HIV-1 IIIb in MT-4 cells, and The IC50 values for AMD-070 are 9-fold higher (0.009 μM vs 0.001 μM) and 8.7-fold higher (0.003 μM vs 0.026 μM) in PBMCs compared to MT-4 cells. AMD-070 has antiviral ability with the IC50 value of 15.5 nM.
In vivo: AMD-070 (2.5 mg/kg, i.v.) shows promising oral bioavailability in rat and dog. The rate of clearance is species dependent with AMD-070 having lower clearance in dog compared to rat.
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Source | PLoS One (2016). Figure 5. AMD-070 |
| Method | IP injections | |
| Cell Lines | murine model of pulmonary fibrosis | |
| Concentrations | 400 μg/animal | |
| Incubation Time | 24 h | |
| Results | When lungs were stained with Masson’s Trichrome stains, there was an average value of 3.7% (SEM ± 1.1) lung fibrosis in the BLM plus acetate buffer control; 10.5% (SEM ±2.5) in the BLM plus AMD070 and 0% (n = 10) in the PBS plus acetate buffer groups respectively |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | PBS |
| Dosages | 50 mg/kg |
| Administration | i.p. |
| Molecular Weight | 349.47 |
| Formula | C21H27N5 |
| CAS Number | 558447-26-0 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CXCR Products |
|---|
| Plerixafor (AMD3100)
Plerixafor (AMD3100) is a CXCR4 chemokine receptor antagonist. |
| WZ 811
WZ811 is a highly competitive CXCR4 antagonist with oral activity. WZ811 effectively inhibited CXCR4/SDF-1 (also known as CXCL12) -mediated regulation of cAMP level (EC50=1.2 nM) and SDF-1-induced matrix glue invasion (EC50=5.2 nM) in cells. |
| Navarixin
Navarixin (SCH 527123) is a novel, selective CXCR2 receptor antagonist with IC50 of 3 nM. Navarixin (SCH 527123) has Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly. |
| AMD3465 hexahydrobromide (AMD3465 )
AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. |
| Plerixafor 8HCl
Plerixafor 8HCl (AMD3100 8HCl) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively. |
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