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PF 06447475
- Soluble in DMSO
- MF: C17H15N5O
- MW: 305.33
Description
PF 06447475 is a potent, selective and brain-penetrant inhibitor of LRRK2 kinase with an IC50 value of 3 nM. It suppresses LRRK2 activity in cellular and in vivo systems and is used to study Parkinson's disease-associated kinase biology.
LRRK2 regulates vesicle trafficking, lysosomal homeostasis, autophagy and neuroinflammatory pathways. PF 06447475 is a useful CNS-active tool for interrogating LRRK2-driven neurodegenerative mechanisms and kinase inhibitor pharmacodynamics.
Key Features
- Brain-penetrant LRRK2 kinase inhibitor
- Reported IC50: 3 nM
- In vivo active and selective LRRK2 pharmacology
- Mitigates neurodegeneration-related phenotypes in reported models
Applications
- LRRK2 and Parkinson's disease research
- CNS kinase inhibitor pharmacology
- Autophagy and lysosomal pathway studies
- Neuroinflammation and neurodegeneration models
More Information
| Parent CAS No. | 1527473-33-1 |
|---|---|
| Chemical Name | 3-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile |
| extra_info | . |
| SMILES | C(#N)C1=CC=CC(C2C3=C(N4CCOCC4)N=CN=C3NC=2)=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C17H15N5O/c18-9-12-2-1-3-13(8-12)14-10-19-16-15(14)17(21-11-20-16)22-4-6-23-7-5-22/h1-3,8,10-11H,4-7H2,(H,19,20,21) |
| InChiKey | BHTWDJBVZQBRKP-UHFFFAOYSA-N |
| CID | 72706840 |
| Short Description | LRRK2 inhibitor |
References
- J.L. Henderson et al. Discovery and preclinical profiling of PF-06447475, a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. J Med Chem. 2015 Jan 8;58(1):419-32.
- J.P. Daher et al. Leucine-rich Repeat Kinase 2 (LRRK2) Pharmacological Inhibition Abates α-Synuclein Gene-induced Neurodegeneration. J Biol Chem. 2015 Aug 7;290(32):19433-44.
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