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Edicotinib
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Catalog No. T15199Cas No. 1142363-52-7
Alias JNJ-527, JNJ-40346527
Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.
Edicotinib
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Purity: 99.72%
Catalog No. T15199Alias JNJ-527, JNJ-40346527Cas No. 1142363-52-7
Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $64 | In Stock | In Stock | |
| 2 mg | $93 | In Stock | In Stock | |
| 5 mg | $155 | In Stock | In Stock | |
| 10 mg | $228 | In Stock | In Stock | |
| 25 mg | $397 | In Stock | In Stock | |
| 50 mg | $583 | In Stock | In Stock | |
| 100 mg | $813 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.72%
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis. |
| Targets&IC50 | c-Kit:20 nM , CSF1R:3.2 nM, FLT3:190 nM |
| In vitro | METHODS: N13 mouse microglial cell line was incubated with Edicotinib (JNJ-527) (0.1, 1, 10, 100, 1000 nM) for 30 min. We characterized the effects of the selective CSF1R inhibitor JNJ-527 on CSF1R activation in vitro. RESULTS Edicotinib (JNJ-527) resulted in a dose-dependent decrease in CSF1R activation and a reduction in ERK1 and ERK2 phosphorylation, with an IC50 of 18.6 nM for CSF1R and 22.5 nM for ERK1/2. [1] |
| In vivo | METHODS: ME7 mice were treated with JNJ-527 (3, 10, 30, 100 mg/kg, oral) for five consecutive days at 12 weeks post-induction (wpi), followed by a dose-response experiment to evaluate the potential of Edicotinib (JNJ-527) to block microglial proliferation in ME7-prion mice. RESULTS Edicotinib (JNJ-527) administered at 30 mg/kg significantly blocked microglial proliferation in ME7-prion mice without altering the population dynamics in the healthy brain. [1] |
| Synonyms | JNJ-527, JNJ-40346527 |
| Molecular Weight | 461.6 |
| Formula | C27H35N5O2 |
| Cas No. | 1142363-52-7 |
| Smiles | CC1(C)CCC(=CC1)c1nc(ccc1NC(=O)c1ncc([nH]1)C#N)C1CC(C)(C)OC(C)(C)C1 |
| Relative Density. | 1.19 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | DMSO: 2.31 mg/mL (5 mM), Sonication is recommended.  | |||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.17 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||
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 stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model 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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