Art. -Nr.: HY-15796

GNE0877

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC₅₀ of 3 nM and a K_i of 0.7 nM. GNE0877 can be used for the research of neuroscience.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.81%
CAS. Nr.: 1374828-69-9
Formel: C₁₄H₁₆F₃N₇
Molecular Weight:339.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE0877 Chemical Structure

CAS. Nr.: 1374828-69-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC₅₀ of 3 nM and a K_i of 0.7 nM. GNE0877 can be used for the research of neuroscience^[1].

IC₅₀ & Target

IC50: 3 nM (LRRK2)^[1]

In Vitro

GNE0877 (1 μM; 10-30 min) shows good cellular potency in human liver microsomes and hepatocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

Human liver microsomes and hepatocytes
Concentration:

1 μM
Incubation Time:

10, 20 and 30 min
Result:

Exibited low turnover and good vitro stability in human liver microsomes and hepatocytes with no glucuronidation.

In Vivo

GNE0877 (10 and 50 mg/kg; i.p. once) inhibits LRRK2 Ser1292 autophosphorylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation^[1]
Dosage:

10 and 50 mg/kg
Administration:

Intraperitoneal injection; 10 and 50 mg/kg once
Result:

Tration-dependently inhibited Ser1292 autophosphorylation with an IC₅₀ of 3 nM.

Chemical Information

CAS. Nr. 1374828-69-9
Appearance Solid
Molecular Weight 339.32
Formel C₁₄H₁₆F₃N₇
Color White to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Hum Mol Genet

GTP binding regulates cellular localization of Parkinson's disease-associated LRRK2. [Abstract]

2017 Jul 15;26(14):2747-2767. PMID: 28453723
Universidad de Granada

2017 Jul 5.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (736.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Estrada AA, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9471 mL	14.7354 mL	29.4707 mL	73.6768 mL
	5 mM	0.5894 mL	2.9471 mL	5.8941 mL	14.7354 mL
	10 mM	0.2947 mL	1.4735 mL	2.9471 mL	7.3677 mL
	15 mM	0.1965 mL	0.9824 mL	1.9647 mL	4.9118 mL
	20 mM	0.1474 mL	0.7368 mL	1.4735 mL	3.6838 mL
	25 mM	0.1179 mL	0.5894 mL	1.1788 mL	2.9471 mL
	30 mM	0.0982 mL	0.4912 mL	0.9824 mL	2.4559 mL
	40 mM	0.0737 mL	0.3684 mL	0.7368 mL	1.8419 mL
	50 mM	0.0589 mL	0.2947 mL	0.5894 mL	1.4735 mL
	60 mM	0.0491 mL	0.2456 mL	0.4912 mL	1.2279 mL
	80 mM	0.0368 mL	0.1842 mL	0.3684 mL	0.9210 mL
	100 mM	0.0295 mL	0.1474 mL	0.2947 mL	0.7368 mL

Keywords

GNE0877

2 Cited Publications

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GNE0877

Kinase Inhibitor Library

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Orally Active Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

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Bioactive Compound Library

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GNE0877

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE0877

Kinase Inhibitor Library

Autophagy Compound Library

Orally Active Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GNE0877

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE0877 Related Classifications

HY-15796 Related Classifications