Edicotinib - CAS:1142363-52-7

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

目录号 : KM4926 CAS No. : 1142363-52-7 纯度 : 98%

Data Sheet 产品使用指南

Edicotinib (JNJ-40346527) 是一种有效的、选择性的、具有血脑通透性和口服活性 CSF-1R 抑制剂，IC₅₀ 为 3.2 nM。Edicotinib 对 KIT 和 FLT3 的抑制作用较小，IC₅₀ 值分别为 20 nM 和 190 nM。Edicotinib 抑制小胶质细胞的扩张，减弱小胶质细胞的增殖和神经退行性变。Edicotinib 可以用于阿尔茨海默病和类风湿性关节炎的研究。

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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Other Forms of Rapamycin:

cFMS Receptor Inhibitor IV In-stock
Edicotinib In-stock

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生物活性

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.

体外研究

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.

Western Blot Analysis

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

体内研究

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 CD45CD11b 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 (CD45CD11bLy6Ccells) with only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high cells) at 100 mg/kg.
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.
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.

Animal Model:	C57BL/6 J (Harlan) mice
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
Dosage:	30 mg/kg; 33 days
Administration:	Oral gavage
Result:	Limited microglial expansion and attenuated behavioural deficits in ME7-prion mice.

分子式

C₂₇H₃₅N₅O₂

分子量

461.60

CAS号

1142363-52-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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。
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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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Other Forms of Rapamycin:

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The dilution calculator equation