2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Amyloid-β
  4. BIIB042

BIIB042 是一种强效、口服有效、可穿透血脑屏障且具有选择性的 γ- 分泌酶 (γ-secretase) 调节剂 (GSM)。BIIB042 可降低细胞内 Aβ42 水平并增加 Aβ38 水平。BIIB042 可显著降低 CF-1 小鼠和 Fischer 大鼠脑内 Aβ42 水平，以及食蟹猴血浆中 Aβ42 水平。BIIB042 可降低 Tg2576 小鼠脑内 Aβ42 水平和 Aβ 斑块负荷。BIIB042 可用于阿尔茨海默病 (AD) 的相关研究[1][2]。

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BIIB042

BIIB042 Chemical Structure

CAS No. : 1257396-73-8

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BIIB042 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BIIB042 is a potent, orally active, brain-penetrant, and selective γ-secretase modulator (GSM). BIIB042 reduces Aβ42 and increases Aβ38 levels in cells. BIIB042 significantly reduces brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. BIIB042 reduces Aβ42 levels and Aβ plaque burden in Tg2576 mice. BIIB042 can be used for alzheimer's disease (AD) research[1][2].

体外研究
(In Vitro)

BIIB042 (compound 10a) 对 COX1 和 COX2 的抑制作用非常弱 (IC50 分别为 35 和 27 μM)，对 hERG 通道的抑制作用也很弱 (IC50 = 15 μM)[1]。
BIIB042 具有良好的细胞渗透性，且不是外排转运蛋白的底物[1]。
BIIB042 在肝微粒体中表现出良好的代谢稳定性，且不抑制主要的细胞色素 P450 酶[1]。
BIIB042 (3-30 μM，20 小时) 对 MC-IXC 细胞中 HES-1 蛋白水平没有影响，表明其选择性作用于淀粉样前体蛋白的加工，而不影响 Notch 信号通路[2]。
BIIB042 (20 小时) 降低了 H4-APP 细胞中 Aβ42 的水平 (IC50 = 64.3 nM)，增加了 Aβ38 的水平 (EC50 = 146 nM)，但对 Aβ40 的水平几乎没有影响[2]。

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

BIIB042 相关抗体:

Western Blot Analysis[2]

Cell Line: MC-IXC cells
Concentration: 3, 10 and 30 μM
Incubation Time: 20 h
Result: Did not alter HES1 protein levels.
体内研究
(In Vivo)

BIIB042 (0-60 mg/kg，口服 (混入饲料)，每日一次，持续 65 天) 可显著提高 Tg2576 小鼠脑内 Aβ38 水平并降低 Aβ42 水平[2]。
BIIB042 (0.3-30 mg/kg，口服 (混入饲料)，每日一次，持续 6 个月) 可显著降低 Tg2576 小鼠脑内 Aβ42 水平，并减少脑实质淀粉样斑块负荷[2]。
BIIB042 (0-100 mg/kg，灌胃，单次给药) 可剂量依赖性地降低 CF-1 小鼠脑和血浆中 Aβ42 水平并升高 Aβ38 水平，表明其具有强效且能穿透血脑屏障的 GSM 特性[2]。

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

Animal Model: Tg2576 mice (5 months old)[2]
Dosage: 0, 3, 10, 30 and 60 mg/kg
Administration: p.o. (in diet), daily for 65 days
Result: Significantly increased Aβ38 levels in brain in a dose-dependent manner.
Significantly decreased Aβ42 levels in brain in a dose-dependent manner.
Showed no significant changes in levels of Aβ40.
Significantly reduced insoluble Aβ42 at 10, 30 and 60 mg/kg compared to vehicle.
Showed no significant changes in insoluble Aβ38.
Animal Model: Tg2576 mice (10 months old)[2]
Dosage: 0.3,1,10 and 30 mg/kg
Administration: p.o. (in diet), daily for 6 months
Result: Significantly reduced soluble and insoluble Aβ42 levels in the brain and plasma at 30 mg/kg.
Significantly reduced parenchymal amyloid plaque burden in both the cortex and hippocampus at 30 mg/kg.
Showed a trend towards increased Aβ levels at 0.3 and 1 mg/kg.
Animal Model: CF-1 mice[2]
Dosage: 0, 3, 10, 30 and 100 mg/kg
Administration: i.g., single dose
Result: Induced significant and dose-dependent decreases in Aβ42 at all tested doses.
Showed a dose-dependent increases in Aβ38 at 10, 30 and 100 mg/kg.
Induced Aβ pharmacodynamic responses in plasma, with similar effects as in brain with decreases in Aβ42, increases in Aβ38 and small changes in Aβ40 at higher doses.
Brain concentrations were approximately 80% of plasma concentrations at the 4 h time point across all doses.
分子量

499.54

Formula

C29H29F4NO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BIIB042 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

BIIB0421257396-73-8BIIB 042BIIB-042γ-secretaseAmyloid-βGamma secretaseβ-amyloid peptideAβAbetaGSMAβ42CF-1 miceTg2576 miceADcynomolgus monkeysFischer ratsInhibitorinhibitorinhibit

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