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
纯度 & 产品资料

纯度: ≥99.0%

COA (170 KB)

产品使用指南 (1538 KB)
参考文献

JNJ-40418677 相关分类

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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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