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PF-06455943 

Cat. No. M28571
PF-06455943  Structure
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Quality Control & Documentation
Biological Activity

PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD).

Chemical Information
Molecular Weight 323.32
Formula C17H14FN5O
CAS Number 1527474-15-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Chi-Hyeon Yoo, et al. ACS Chem Neurosci. Evaluation of [18F]PF-06455943 as a Potential LRRK2 PET Imaging Agent in the Brain of Nonhuman Primates

[2] Zhen Chen, et al. J Med Chem. Imaging Leucine-Rich Repeat Kinase 2 In Vivo with 18F-Labeled Positron Emission Tomography Ligand

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CZC-25146 hydrochloride

CZC-25146 is a potent selective and metabolically stable inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson’s disease.

  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06455943  supplier, LRRK2, inhibitors, activators


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