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PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $61 | In Stock | |
25 mg | $89 | In Stock | |
50 mg | $133 | In Stock | |
100 mg | $225 | In Stock | |
200 mg | $397 | In Stock | |
1 mL x 10 mM (in DMSO) | $48 | In Stock |
Description | PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively. |
Targets&IC50 | LRRK2:3nM, LRRK2 (G2019S):11nM |
In vitro | In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. [2] In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function. [3] |
In vivo | In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. [1] In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression. [2] |
Molecular Weight | 305.33 |
Formula | C17H15N5O |
Cas No. | 1527473-33-1 |
Smiles | N#Cc1cccc(c1)-c1c[nH]c2ncnc(N3CCOCC3)c12 |
Relative Density. | 1.40 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 15.3 mg/mL (50 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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