Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with anIC₅₀of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT andFLT3withIC₅₀values 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: 3.2 nM (CSF-1R)^[1]
20 nM (KIT); 190 nM (FLT3)^[2]

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 IC₅₀values are 18.6 nM and 22.5 nM for CSF1R and ERK1/2, respectively^[1].

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⁺CD11b^highLy6C^{intermediate/low}cells) 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 EC₅₀of 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].

461.60

Solid

C₂₇H₃₅N₅O₂

1142363-52-7

Room temperature in continental US; may vary elsewhere.

DMSO : 16.67 mg/mL(36.11 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 17% Polyethylene glycol 12-hydroxystearate in saline

  Solubility: 10 mg/mL (21.66 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

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

  此方案可获得 ≥ 1.67 mg/mL (3.62 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

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

  此方案可获得 ≥ 1.67 mg/mL (3.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。