GNE0877

Potent and selective LRRK2 inhibitor CAS# 1374828-69-9

GNE0877

Catalog No. BCC5369----Order now to get a substantial discount!

Product Name & Size Price Stock
GNE0877: 5mg $184 In Stock
GNE0877: 10mg Please Inquire In Stock
GNE0877: 20mg Please Inquire Please Inquire
GNE0877: 50mg Please Inquire Please Inquire
GNE0877: 100mg Please Inquire Please Inquire
GNE0877: 200mg Please Inquire Please Inquire
GNE0877: 500mg Please Inquire Please Inquire
GNE0877: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of GNE0877

Number of papers citing our products

Chemical structure

GNE0877

3D structure

Chemical Properties of GNE0877

Cas No. 1374828-69-9 SDF Download SDF
PubChem ID 69093374 Appearance Powder
Formula C14H16F3N7 M.Wt 339.32
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 2-methyl-2-[3-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]pyrazol-1-yl]propanenitrile
SMILES CC1=NN(C=C1NC2=NC=C(C(=N2)NC)C(F)(F)F)C(C)(C)C#N
Standard InChIKey ZPPUMAMZIMPJGP-UHFFFAOYSA-N
Standard InChI InChI=1S/C14H16F3N7/c1-8-10(6-24(23-8)13(2,3)7-18)21-12-20-5-9(14(15,16)17)11(19-4)22-12/h5-6H,1-4H3,(H2,19,20,21,22)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GNE0877

DescriptionGNE-0877 is a highly potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with Ki value of 0.7 nM.
TargetsLRRK2    
IC50Ki=0.7 nM     

GNE0877 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

GNE0877 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of GNE0877

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9471 mL 14.7354 mL 29.4707 mL 58.9414 mL 73.6768 mL
5 mM 0.5894 mL 2.9471 mL 5.8941 mL 11.7883 mL 14.7354 mL
10 mM 0.2947 mL 1.4735 mL 2.9471 mL 5.8941 mL 7.3677 mL
50 mM 0.0589 mL 0.2947 mL 0.5894 mL 1.1788 mL 1.4735 mL
100 mM 0.0295 mL 0.1474 mL 0.2947 mL 0.5894 mL 0.7368 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on GNE0877

Leucine-rich repeat kinase 2 (LRRK2) has drawn significant interest in the neuroscience research community because it is one of the most compelling targets for a potential disease-modifying Parkinson’s disease therapy. GNE-0877 is a highly potent and selective LRRK2 inhibitors.

In vitro: GNE-0877 showed significantly enhanced LRRK2 cellular potency (3 nM) and low turnover in human liver microsomes and hepatocytes with no evidence of glucuronidation. Invitrogen kinase-selectivity profiling (188 kinases) of GNE-0877 at 0.1 μM resulted in only four kinases showing greater than 50% inhibition and suggested that GNE-0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE-0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki = 150 nM) [1].

In vivo: GNE-0877 was evaluated for its ability to inhibit in vivo LRRK2 Ser1292 autophosphorylation using BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation. Using free-drug concentrations, robust concentration-dependent inhibition of Ser1292 autophosphorylation was observed for GNE-0877 [1].

Clinical trials: Currenlty no clinical data are available.

Reference:
[1] Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK.   Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36.

Featured Products
New Products
 

Description

GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.

Keywords:

GNE0877,1374828-69-9,Natural Products,LRRK2, buy GNE0877 , GNE0877 supplier , purchase GNE0877 , GNE0877 cost , GNE0877 manufacturer , order GNE0877 , high purity GNE0877

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: