2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Amyloid-β
  4. JNJ-40418677

JNJ-40418677 是一种具有口服活性的 γ-分泌酶调节剂，可通过血脑屏障。JNJ-40418677 抑制 Aβ42 淀粉样蛋白和 NS2B-NS3 蛋白酶，IC50 分别为 200 nM 和 3.9 μM。JNJ-40418677 表现出良好的生物耐受性，可用于阿尔茨海默症的研究。

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JNJ-40418677 Chemical Structure

JNJ-40418677 Chemical Structure

CAS No. : 1146594-87-7

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5 mg ￥3900
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JNJ-40418677 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC50s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research[1][2][3].

IC50 & Target

IC50: 185 nM (rat Aβ42)[1]; 200 nM (human Aβ42)[2]; 3.9 μM (ZIKV NS2B-NS3 protease)[3]
体外研究
(In Vitro)

JNJ-40418677 (0.2 nM-0.3 mM; 16 h) selectively reduces Aβ42 secretion in cell culture supernatants of human neuroblastoma cells with mean IC50 of 200 nM and (0.2 nM-0.3 mM; 48 h) of rat primary neurons with mean IC50 of 185 nM[1].
JNJ-40418677 (10 μM, 100 μM; 18 h) does not inhibit Notch processing or (6 nM-20 μM; 18 h) not affect formation of other amyloid precursor protein cleavage (CTF-β, CTF-α) products, and shows no inhibitory activity against COX-1/2 at a high concentration of 60 μM[1].
JNJ-40418677 suppresses ZIKV in human neuronal stem cells with an EC50 value of 3.2 μM, and inhibits ZIKV NS2B-NS3 protease with an IC50 value of 3.9 μM[3].

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

JNJ-40418677 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 10 μM
Incubation Time: 18 h
Result: Resulted Aβ42 decreasing, Aβ38 increasing and Aβ40 levels remained unchanged.
体内研究
(In Vivo)

JNJ-40418677 (10-300 mg/kg; p.o.) decreases Aβ42 brain levels in a dose-dependent manner 4 h after treatment, while increasing Aβ38 level in non-transgenic mouse brain[1].
JNJ-40418677 (30 mg/kg; p.o.; once) shows the mean brain and plasma levels 4 h after single dose are both 17 μM, indicating good brain penetration in non-transgenic mouse brain[1].
JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) has good biological tolerance with no adverse effects in a chronic treatment in Tg2576 mice[1].
JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) decreases the plaque number and the area occupied by plaques in Tg2576 mice dose-dependently[1].

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

Animal Model: Non-transgenic mouse (6-month-old)[1]
Dosage: 10, 30, 100, 300 mg/kg
Administration: Oral gavage; once
Result: Reduced the Aβ42 brain levels dose-dependently, with 82%, 64%, 39%, and 31% at the doses of 10, 30, 100, 300 mg/kg, respectively.
Animal Model: Tg2576 mice (6-month-old)[1]
Dosage: 20, 60, 120 mg/kg
Administration: Oral gavage; 7 months
Result: Exhibited well tolerated activity, without adverse effects on body weight.
Showed no influence on the steady state levels of full-length APP, CTF-a, and CTF-b at a dosage of 120 mg/kg.
Significantly reduced plaque area fraction and number of plaques.
分子量

480.44

Formula

C26H22F6O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 10 mg/mL (20.81 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0814 mL 10.4071 mL 20.8143 mL
5 mM 0.4163 mL 2.0814 mL 4.1629 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

COA (263 KB)

产品使用指南 (1538 KB)
参考文献

JNJ-40418677 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0814 mL 10.4071 mL 20.8143 mL 52.0356 mL
5 mM 0.4163 mL 2.0814 mL 4.1629 mL 10.4071 mL
10 mM 0.2081 mL 1.0407 mL 2.0814 mL 5.2036 mL
15 mM 0.1388 mL 0.6938 mL 1.3876 mL 3.4690 mL
20 mM 0.1041 mL 0.5204 mL 1.0407 mL 2.6018 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-404186771146594-87-7JNJ40418677JNJ 40418677γ-secretaseAmyloid-βGamma secretaseβ-amyloid peptideAβAbetaAlzheimer’s diseaseamyloid plaque formationamyloid β42neurotoxichuman neuroblastoma cellsrat primary neuronsSKNBE-2 cellsflavivirusNS2B-NS3 proteaseZIKVInhibitorinhibitorinhibit

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