pf 475  (MedChemExpress)

Journal: iScience

Article Title: Rebalance of mitophagy by inhibiting LRRK2 improves colon alterations in an MPTP in vivo model

doi: 10.1016/j.isci.2024.110980

Figure Lengend Snippet:

Article Snippet: PF06447475 (abbreviated as PF-475) was purchased from MedChemExpress LLC (1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA; # HY-12477).

Techniques: Recombinant, Enzyme-linked Immunosorbent Assay, Software

Journal: iScience

Article Title: Rebalance of mitophagy by inhibiting LRRK2 improves colon alterations in an MPTP in vivo model

doi: 10.1016/j.isci.2024.110980

Figure Lengend Snippet:

Article Snippet: PF06447475 , MedChemExpress LLC , HY-12477.

Techniques: Recombinant, Enzyme-linked Immunosorbent Assay, Software

Journal: Journal of Medicinal Chemistry

Article Title: Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2)

doi: 10.1021/acs.jmedchem.3c01687

Figure Lengend Snippet: Representative LRRK2 PET tracers: (A) previous work; (B) this work.

Article Snippet: Toward this end, we were enlightened by PF-06447475 ( 3 ), an LRRK2 inhibitor lead initially disclosed by Pfizer.

Techniques:

Journal: Journal of Medicinal Chemistry

Article Title: Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2)

doi: 10.1021/acs.jmedchem.3c01687

Figure Lengend Snippet: Validation of [ 18 F] 4 in LRRK2-G2019S mutant and wild-type (WT) mice. (A) Representative PET images (0–10 min summed); (B) representative Western blot images; (C) quantitative analysis of area under curves for PET imaging studies; and (D) quantitative analysis of LRRK2 enzyme density. Asterisks indicate the statistical significance. ** p ≤ 0.01 and *** p ≤ 0.001.

Article Snippet: Toward this end, we were enlightened by PF-06447475 ( 3 ), an LRRK2 inhibitor lead initially disclosed by Pfizer.

Techniques: Biomarker Discovery, Mutagenesis, Western Blot, Imaging

Journal: Journal of Medicinal Chemistry

Article Title: Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2)

doi: 10.1021/acs.jmedchem.3c01687

Figure Lengend Snippet: Validation of [ 18 F] 4 in LPS mice. (A) Representative PET images in LPS, sham, and baseline mice (0–15 min summed); (B) representative Western blot images. Quantitative analysis of (C) area under curves and (D) LRRK2 enzyme density. Asterisks indicate the statistical significance. * p ≤ 0.05, ** p ≤ 0.01, *** p ≤ 0.001, and **** p ≤ 0.0001.

Article Snippet: Toward this end, we were enlightened by PF-06447475 ( 3 ), an LRRK2 inhibitor lead initially disclosed by Pfizer.

Techniques: Biomarker Discovery, Western Blot

Journal: Journal of Medicinal Chemistry

Article Title: Preclinical Evaluation of Novel Positron Emission Tomography (PET) Probes for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2)

doi: 10.1021/acs.jmedchem.3c01687

Figure Lengend Snippet: Comparison of the Pharmacological and Pharmacokinetic Properties of Representative LRRK2 Inhibitors 15 , 18 , 23 , 24

Article Snippet: Toward this end, we were enlightened by PF-06447475 ( 3 ), an LRRK2 inhibitor lead initially disclosed by Pfizer.

Techniques: Comparison

Journal: CNS Neuroscience & Therapeutics

Article Title: Efficacy of a benzothiazole‐based LRRK2 inhibitor in oligodendrocyte precursor cells and in a murine model of multiple sclerosis

doi: 10.1111/cns.14552

Figure Lengend Snippet: The inhibition of LRRK2 by PF‐475 and compound 4 promotes the proliferation of OPCs from rat brain cortices. (A) Representative images of OPCs cultures treated for 24 h with PF‐475 (0.1 μM) and 4 (1 and 5 μM) 6 h with BrdU, the number of BrdU + Olig2 + was measured. (B) Quantification of proliferating OPCs (BrdU + /Olig2 + double staining) was performed in respect to the total number of oligodendroglial cells (Olig2 + ) for LRRK2 inhibitors PF‐475 and compounds 1–5. Values represent the mean ± SEM of three replications in five different experiments. Results of Student's t ‐test are represented as: * p < 0.05 versus control. The scale bar represents 25 μm in A–D.

Article Snippet: The inhibitor PF‐06447475 (PF‐475) was obtained from Sigma‐Aldrich.

Techniques: Inhibition, Double Staining