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RXP470.1

Cat. No. M42514
RXP470.1 Structure
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Biological Activity

RXP470.1 (RXP-470) is a potent, selective MMP-12 inhibitor with a Ki of 0.2 nM against human MMP-12.

Chemical Information
Molecular Weight 818
Formula C35H35BrClN4O10P
CAS Number 891198-31-5
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] Laurent Devel et al. Molecules. Biodistribution of Nanostructured Lipid Carriers in Mice Atherosclerotic Model

[2] Mahmoud Razavian et al. Sci Rep. Optical imaging of MMP-12 active form in inflammation and aneurysm

[3] Thomas Bordenave et al. Bioconjug Chem. Synthesis and in Vitro and in Vivo Evaluation of MMP-12 Selective Optical Probes

[4] Bertrand Czarny et al. J Med Chem. Molecular determinants of a selective matrix metalloprotease-12 inhibitor: insights from crystallography and thermodynamic studies

[5] Jason L Johnson et al. Arterioscler Thromb Vasc Biol. A selective matrix metalloproteinase-12 inhibitor retards atherosclerotic plaque development in apolipoprotein E-knockout mice

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Keywords: RXP470.1 supplier, MMP, inhibitors, activators


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