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GNE-7915

Item № 16252
CAS № 1351761-44-8
Purity ≥98%
product image
                (CAS 1351761-44-8)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $65.00 0.00
     10 mg $124.00 0.00
     50 mg $455.00 0.00

Pricing updated 2019-05-26. Prices are subject to change without notice.

Description

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson's disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE-7915 is a selective, brain-penetrable LRRK2 inhibitor (Kis = 2 and 18.7 nM in biochemical and cell-based assays, respectively).1 It inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC50 value of 20 nM in vivo.1

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Technical Information
Formal Name
[4-[[4-(ethylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2-fluoro-5-methoxyphenyl]-4-morpholinyl-methanone
CAS Number
1351761-44-8
Molecular Formula
C19H21F4N5O3
Formula Weight
443.4
Purity
≥98%
Formulation
A crystalline solid
λmax
255, 314 nm
SMILES
CCNC1=C(C(F)(F)F)C=NC(NC2=CC(F)=C(C(N3CCOCC3)=O)C=C2OC)=N1
InChI Code
InChI=1S/C19H21F4N5O3/c1-3-24-16-12(19(21,22)23)10-25-18(27-16)26-14-9-13(20)11(8-15(14)30-2)17(29)28-4-6-31-7-5-28/h8-10H,3-7H2,1-2H3,(H2,24,25,26,27)
InChI Key
XCFLWTZSJYBCPF-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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References & Product Citations
Product Description References

1. Estrada, A.A., Chan, B.K., Baker-Glenn, C., et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors Journal of Medicinal Chemistry 57(3), 921-936 (2014).

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