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PSB-12379

Cat. No. M11275
PSB-12379  Structure
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Biological Activity

Psb-12379 is a nucleotide analogue and a potent ECTO-5 '-nucleotidase (CD73) inhibitor with Kis values of 9.03 nM (rat) and 2.21 nM (human).

Chemical Information
Molecular Weight 515.35
Formula C18H23N5O9P2
CAS Number 1802226-78-3
Solubility (25°C) Water ≥ 100 mg/mL
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] Gabor Viczjan, et al. Int J Mol Sci. A Body of Circumstantial Evidence for the Irreversible Ectonucleotidase Inhibitory Action of FSCPX, an Agent Known as a Selective Irreversible A 1 Adenosine Receptor Antagonist So Far

[2] Constanze C Schmies, et al. ACS Med Chem Lett. Fluorescent Probes for Ecto-5'-nucleotidase (CD73)

[3] Sanjay Bhattarai, et al. J Med Chem. α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5'-Nucleotidase (CD73) Inhibitors

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