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PF-06447475

Cat. No. M3929
PF-06447475 Structure
Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
25mg USD 135  USD135 In stock
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Quality Control
Biological Activity

PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. PF-06447475 was sufficiently potent in the LRRK2 whole cell assay (WCA; IC50=25 nM) (pS935 end point) to warrant additional profiling. Oral administration of PF-06447475 twice daily for 15 days was well tolerated at doses up to 60 mg kg-1 day-1 (31-fold Cave,0.24h; 70-fold Cmax) with only minimal alterations in RBC parameters, electrolytes, and food consumption without concurrent effects on body weight.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models G2019S BAC-transgenic mice
Formulation 10% propylene glycol/20% PEG400/70% 9.5% methocellulose
Dosages 100 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 305.33
Formula C17H15N5O
CAS Number 1527473-33-1
Purity 99.42%
Solubility DMSO 30 mg/mL
Storage at -20°C
References

[1] Henderson JL, et al. J Med Chem. Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-06447475 supplier, LRRK2, inhibitors

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