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ONO-8430506

Cat. No. M21275
ONO-8430506  Structure
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Biological Activity

ONO-8430506 is a potent autotaxin phosphodiesterase inhibitor with significant oral exposure and low clearance in higher species.

Chemical Information
Molecular Weight 461.53
Formula C27H28FN3O3
CAS Number 1354805-08-5
Solubility (25°C) N/A
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] Baasanjav Uranbileg, et al. Sci Rep. Inhibition of autotaxin activity ameliorates neuropathic pain derived from lumbar spinal canal stenosis

[2] Yuzo Iwaki, et al. ACS Med Chem Lett. ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model

[3] Matthew G K Benesch, et al. Endocr Relat Cancer. Autotaxin is an inflammatory mediator and therapeutic target in thyroid cancer

[4] Matthew G K Benesch, et al. J Lipid Res. Regulation of autotaxin expression and secretion by lysophosphatidate and sphingosine 1-phosphate

[5] Matthew G K Benesch, et al. FASEB J. Inhibition of autotaxin delays breast tumor growth and lung metastasis in mice

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  Catalog
Abmole Inhibitor Catalog




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