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PF-05180999

Cat. No. M28318
PF-05180999 Structure
Synonym:

PF-999

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Biological Activity

PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.

Chemical Information
Molecular Weight 414.39
Formula C19H17F3N8
CAS Number 1394033-54-5
Form Solid
Solubility (25°C) DMSO 50 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] Yuqing Yan, et al. Int J Neuropsychopharmacol. Characterization of 2 Novel Phosphodiesterase 2 Inhibitors Hcyb1 and PF-05180999 on Depression- and Anxiety-Like Behavior

[2] Guibao Gu, et al. J Pharmacol Exp Ther. Target Engagement of a Phosphodiesterase 2A Inhibitor Affecting Long-Term Memory in the Rat

[3] Jie Chen, et al. Neurochem Int. Effect of phosphodiesterase (1B, 2A, 9A and 10A) inhibitors on central nervous system cyclic nucleotide levels in rats and mice

[4] Christopher J Helal, et al. J Med Chem. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate

[5] Laigao Chen, et al. J Nucl Med. Preclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme

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Keywords: PF-05180999, PF-999 supplier, PDE, inhibitors, activators


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