1. Autophagy
  2. LRRK2
  3. PF-06447475

PF-06447475 

Cat. No.: HY-12477 Purity: 99.88%
Handling Instructions

PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.

For research use only. We do not sell to patients.

PF-06447475 Chemical Structure

PF-06447475 Chemical Structure

CAS No. : 1527473-33-1

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Based on 1 publication(s) in Google Scholar

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Description

PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.

IC50 & Target

IC50: 3 nM (LRRK2)[1].

In Vitro

PF-06447475 inhibits LRRK2 enzyme and LRRK2 in the whole cell assay with IC50s of 3 and 25 nM, respectively[1]. Cells incubated with PF-06447475 alone (0.5, 1, 3 μM) or in the presence of ROT significantly reduces (S935)-LRRK2 kinase phosphorylation to control. PF-06447475 significantly preserves the nucleus morphology and ΔΨm of NLCs exposed to ROT compared to untreated and control. PF-475 significantly diminishes ROT-induced ROS generation to a similar extent to cells exposed to PF-475 alone[2].

In Vivo

In G2019S+ rats treated with PF-06447475, a significant reduction in microgliosis to levels found in wild-type rats could be observed. The proinflammatory marker MHC-II expressed on myeloid cells but not neurons also appears to be less abundant in confocal sections in G2019S+ rats treated with PF-06447475. PF-06447475 treatment in G2019S+ rats significantly lowers the number of CD68 cells recruited to the SNpc. PF-06447475 successfully blocks the enhanced neuroinflammation associated with G2019S-LRRK2 expression. Treatment of G2019S+ rats with PF-06447475 preserves TH expression in the dorsal striatum, consistent with drug attenuating neurodegeneration in the SNpc[3]. PF-06447475 is well tolerated in rats[1].

Molecular Weight

305.33

Formula

C₁₇H₁₅N₅O

CAS No.

1527473-33-1

SMILES

N#CC1=CC=CC(C2=CNC3=NC=NC(N4CCOCC4)=C32)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (108.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2751 mL 16.3757 mL 32.7515 mL
5 mM 0.6550 mL 3.2751 mL 6.5503 mL
10 mM 0.3275 mL 1.6376 mL 3.2751 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

Rats: PF-06447475 are administered to the desired amount in a suspension solution consisting of 10% propylene glycol, 20% PEG-400, and 70% 0.5% methylcellulose. To determine the potency of PF-06447475 in blocking brain LRRK2 kinase activity, wild-type Sprague-Dawley rats are treated at 3 and 30 mg/kg PF-06447475 (p.o. b.i.d.) for 14 days, and total and phospho-LRRK2 are subsequently measured from brain tissue lysates[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.88%

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Keywords:

PF-06447475PF06447475PF 06447475LRRK2Leucine-rich repeat kinase 2Inhibitorinhibitorinhibit

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PF-06447475
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HY-12477
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