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GNE0877
Catalog No. T6031Cas No. 1374828-69-9
Alias GNE-0877, GNE 0877
GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).
GNE0877
Catalog No. T6031Alias GNE-0877, GNE 0877Cas No. 1374828-69-9
GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $39 | In Stock | |
| 2 mg | $55 | In Stock | |
| 5 mg | $122 | In Stock | |
| 10 mg | $197 | In Stock | |
| 25 mg | $396 | In Stock | |
| 50 mg | $592 | In Stock | |
| 100 mg | $845 | In Stock | |
| 500 mg | $1,730 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock |
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CZC-54252 hydrochloride is a selective inhibitor of LRRK2 with IC50s of 1.85 nM and 1.28 nM for wild-type and G2019S LRRK2. CZC-54252 hydrochloride has a neuroprotective activity and attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of 1 nM.
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Purity:99.96%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM). |
| Targets&IC50 | LRRK2:0.7 nM(Ki) |
| In vitro | Within BAC transgenic mice expressing human LRRK2 protein with the Parkinson's disease mutation G2019S, GNE-0877 effectively inhibits LRRK2 Ser1292 autophosphorylation. GNE-0877 demonstrates favorable oral bioavailability and brain penetrance. |
| In vivo | GNE-0877 significantly inhibits LRRK2 cellular activity (IC50: 3 nM) and demonstrates low turnover in human liver microsomes and hepatocytes. Additionally, GNE-0877 acts as a reversible inhibitor of CYP1A2 (IC50: 0.7 μM). |
| Alias | GNE-0877, GNE 0877 |
| Molecular Weight | 339.32 |
| Formula | C14H16F3N7 |
| Cas No. | 1374828-69-9 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (132.62 mM)  H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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