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AMD-070

Cat. No. M6217
AMD-070 Structure
Synonym:

mavorixafor

Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 280  USD280 In stock
50mg USD 850  USD850 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Protocol (for reference only)
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Chow LN, et al. PLoS One. Impact of a CXCL12/CXCR4 Antagonist in Bleomycin (BLM) Induced Pulmonary Fibrosis and Carbon Tetrachloride (CCl4) Induced Hepatic Fibrosis in Mice.

[2] Zhang C, et al. Chem Biol Drug Des. Hologram quantitative structure activity relationship, docking, and molecular dynamics studies of inhibitors for CXCR4.

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Keywords: AMD-070, mavorixafor supplier, CXCR, inhibitors, activators


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