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  3. GNE0877

GNE0877 

Cat. No.: HY-15796 Purity: 98.07%
Handling Instructions

GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.

For research use only. We do not sell to patients.

GNE0877 Chemical Structure

GNE0877 Chemical Structure

CAS No. : 1374828-69-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 168 In-stock
Estimated Time of Arrival: December 31
2 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 980 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM. IC50 value: 3 nM [1] Target: LRRK2 Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in the maintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension.

Molecular Weight

339.32

Formula

C₁₄H₁₆F₃N₇

CAS No.

1374828-69-9

SMILES

CC1=NN(C(C)(C)C#N)C=C1NC2=NC=C(C(F)(F)F)C(NC)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (73.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9471 mL 14.7354 mL 29.4707 mL
5 mM 0.5894 mL 2.9471 mL 5.8941 mL
10 mM 0.2947 mL 1.4735 mL 2.9471 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GNE0877GNE 0877GNE-0877LRRK2Leucine-rich repeat kinase 2Inhibitorinhibitorinhibit

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GNE0877
Cat. No.:
HY-15796
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