1351761-44-8 Usage
Description
GNE 7915 is a selective, brain-penetrable small molecule inhibitor of Leucine-Rich Repeat Kinase 2 (LRRK2), an enzyme associated with Parkinson's disease. It effectively inhibits LRRK2 Ser1292 autophosphorylation and has demonstrated the ability to penetrate the Blood-Brain Barrier (BBB), making it a promising candidate for the treatment of Parkinson's disease.
Uses
Used in Pharmaceutical Industry:
GNE 7915 is used as a therapeutic agent for the treatment of Parkinson's disease. It targets the LRRK2 enzyme, which is linked to the development and progression of the disease, and has shown potential in reducing dopaminergic cell death by inhibiting the increased kinase activity associated with LRRK2 gene mutations.
Used in Research and Development:
GNE 7915 is used as a research tool for studying the role of LRRK2 in Parkinson's disease and for developing new therapeutic strategies targeting this enzyme. Its ability to penetrate the BBB and selectively inhibit LRRK2 makes it a valuable compound for exploring the underlying mechanisms of the disease and evaluating the potential of LRRK2 inhibition as a treatment approach.
Check Digit Verification of cas no
The CAS Registry Mumber 1351761-44-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,5,1,7,6 and 1 respectively; the second part has 2 digits, 4 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1351761-44:
(9*1)+(8*3)+(7*5)+(6*1)+(5*7)+(4*6)+(3*1)+(2*4)+(1*4)=148
148 % 10 = 8
So 1351761-44-8 is a valid CAS Registry Number.
1351761-44-8Relevant articles and documents
The tale of proteolysis targeting chimeras (PROTACs) for Leucine-Rich Repeat Kinase 2 (LRRK2)
Konstantinidou, Markella,Oun, Asmaa,Pathak, Pragya,Zhang, Bidong,Wang, Zefeng,ter Brake, Frans,Dolga, Amalia M.,Kortholt, Arjan,D?mling, Alexander
, p. 959 - 965 (2020/12/30)
Here we present the rational design and synthetic methodologies towards proteolysis-targeting chimeras (PROTACs) for the recently-emerged target leucine-rich repeat kinase 2 (LRRK2). Two highly potent, selective, brain-penetrating kinase inhibitors were selected, and their structure was appropriately modified to assemble a cereblon-targeting PROTAC. Biological data show strong kinase inhibition and the ability of the synthesized compounds to enter the cells. However, data regarding the degradation of the target protein are inconclusive. The reasons for the inefficient degradation of the target are further discussed.
AMINOPYRIMIDINE DERIVATIVES AS LRRK2 INHIBITORS
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Page/Page column 72, (2011/12/14)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compound
