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ATX inhibitor 18

Cat. No. M42562
ATX inhibitor 18 Structure
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Biological Activity

ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM.

Chemical Information
Molecular Weight 459.3
Formula C21H17Cl2FN6O
CAS Number 2402772-30-7
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] Edris Ebrahimi et al. Bioorg Med Chem Lett. [18F]ONO-8430506: A novel radioligand for PET imaging of autotaxin (ATX)

[2] Hui-Li Yang et al. Autophagy. A defective lysophosphatidic acid-autophagy axis increases miscarriage risk by restricting decidual macrophage residence

[3] Xiaoyun Deng et al. J Med Chem. Imaging Autotaxin In Vivo with 18F-Labeled Positron Emission Tomography Ligands

[4] Marcus Litchfield et al. Mol Pharm. Positron Emission Tomography Imaging of Autotaxin in Thyroid and Breast Cancer Models Using [18F]PRIMATX

[5] Anand Balupuri et al. Eur J Med Chem. Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation

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