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Edicotinib (Synonyms: JNJ-40346527; JNJ-527)

Cat. No.: HY-109086 Purity: 99.56%
Handling Instructions

Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.

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

Edicotinib Chemical Structure

Edicotinib Chemical Structure

CAS No. : 1142363-52-7

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10 mM * 1 mL in DMSO USD 231 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 350 In-stock
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25 mg USD 750 In-stock
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50 mg USD 1100 In-stock
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100 mg USD 1800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively[1]. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research[1][2].

IC50 & Target

IC50: 3.2 nM (CSF-1R)[1]
20 nM (KIT); 190 nM (FLT3)[2]

In Vitro

Edicotinib (0.1 nM-1μM; 24 hours) Leads to a dose-dependent decrease of CSF1R activation and a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose response curve shows the effect of JNJ-527 on CSF1R and ERK1/2, and the IC50 values are 18.6 nM and 22.5 nM for CSF1R and ERK1/2, respectively[1].

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

Western Blot Analysis[1]

Cell Line: N13 microglial cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 24 hours
Result: Prevented CSF1R and ERK1/2 phosphorylation in N13 microglial cells
In Vivo

Edicotinib (oral gavage; 3, 10, 30 and 100 mg/kg; 5 days) significantly inhibits microglial proliferation in ME7 mice. It diminishes the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg, and JNJ-527 depletes up to 50% of patrolling blood monocytes at every dose tested (CD45+CD11bhighLy6Cintermediate/lowcells) with only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high cells) at 100 mg/kg[1].
Edicotinib exhibits a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively[1].
Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced,but not other inflammatory cytokines[1].

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

Animal Model: C57BL/6 J (Harlan) mice[1] 
Dosage: 3, 10, 30 and 100 mg/kg; 5 days
Administration: Oral gavage
Result: Did not affect microglial numbers when administered under 100 mg/kg.
Animal Model: C57BL/6 J (Harlan) mice[1] 
Dosage: 30 mg/kg; 33 days
Administration: Oral gavage
Result: Limited microglial expansion and attenuated behavioural deficits in ME7-prion mice.
Clinical Trial
Molecular Weight

461.60

Formula

C₂₇H₃₅N₅O₂

CAS No.
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 : 16.67 mg/mL (36.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1664 mL 10.8319 mL 21.6638 mL
5 mM 0.4333 mL 2.1664 mL 4.3328 mL
10 mM 0.2166 mL 1.0832 mL 2.1664 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  17% Polyethylene glycol 12-hydroxystearate in saline

    Solubility: 10 mg/mL (21.66 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 1.67 mg/mL (3.62 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.67 mg/mL (3.62 mM); Clear solution

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

Purity: 99.56%

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Edicotinib
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