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AMG 579 

Cat. No. M27983
AMG 579  Structure
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Biological Activity

AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.

Chemical Information
Molecular Weight 441.48
Formula C25H23N5O3
CAS Number 1227067-61-9
Form Solid
Solubility (25°C) DMSO 41.67 mg/mL (ultrasonic)
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] Damian P Hruszkewycz, et al. Chem Sci. Co/NHPI-mediated aerobic oxygenation of benzylic C-H bonds in pharmaceutically relevant molecules

[2] Qiong Wu, et al. Int J Pharm. Humidity induced phase transformation of poloxamer 188 and its effect on physical stability of amorphous solid dispersion of AMG 579, a PDE10A inhibitor

[3] Sarah F Wilson, et al. J Pharm Biomed Anal. Validation of a method for the determination of AMG 579 in cerebrospinal fluid with a focus on sample collection procedures for clinical trials

[4] Essa Hu, et al. J Med Chem. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A)

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Keywords: AMG 579  supplier, PDE, inhibitors, activators


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