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PBD-150

Cat. No. M20810
PBD-150 Structure
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Biological Activity

PBD-150 is a potent human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor with Ki of 60 nM.

Chemical Information
Molecular Weight 320.41
Formula C15H20N4O2S
CAS Number 790663-33-1
Solubility (25°C) DMSO 64 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] Flavio DiPisa, et al. Acta Crystallogr F Struct Biol Commun. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease

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  Catalog
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