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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 |
|---|
| Elubrixin
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
| VUF 11222
VUF 11222 is a CXCR3 non-peptide-like agonist. |
| (±)-AMG 487
(±)-AMG 487 is a racemate of AMG 487. |
| Elubrixin tosylate
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
| Elubrixin hydrochloride
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. |
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