GNE0877Potent and selective LRRK2 inhibitor CAS# 1374828-69-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
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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. |
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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. |
Description | GNE-0877 is a highly potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with Ki value of 0.7 nM. | |||||
Targets | LRRK2 | |||||
IC50 | Ki=0.7 nM |
GNE0877 Dilution Calculator
GNE0877 Molarity Calculator
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. |
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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.
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