2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Amyloid-β
  4. BMS-869780

BMS-869780 是一类具有口服活性的非酸性 γ-分泌酶 (γ-secretase) 调节剂。BMS-869780 可调控 γ-分泌酶的活性，从而改变 β-淀粉样蛋白的生成谱，单独作用时可改变特定 β-淀粉样蛋白亚型的相对水平，而不会抑制 β-淀粉样蛋白的总生成量。BMS-869780 与酸性结构类 γ-分泌酶调节剂具有协同作用，可在细胞培养物中抑制 β-淀粉样蛋白的总生成量。

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BMS-869780

BMS-869780 Chemical Structure

CAS No. : 1235493-78-3

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BMS-869780 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

BMS-869780 is an orally active non-acidic γ-secretase (γ-secretase) modulator. BMS-869780 regulates the activity of γ-secretase, thereby altering the production profile of β-amyloid proteins. When acting alone, it changes the relative levels of specific β-amyloid subtypes without inhibiting the total production of β-amyloid proteins. BMS-869780 exerts a synergistic effect with γ-secretase modulators of the acidic structural class to inhibit the total production of β-amyloid proteins in cell cultures[1].

体外研究
(In Vitro)

BMS-869780 单独作用时不会抑制总 Aβ 的生成，但在人神经胶质瘤 H4-APPsw 细胞中与酸性 GSM (GSM-2 或 GSM-1 (HY-119165)) 联用时，对 Aβ1-x 和 Aβ1-40 的生成表现出强烈的协同抑制作用 (联合指数值低至 0.05-0.06)，并可诱导 α-CTF 的积累[1]。

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

BMS-869780 相关抗体:
体内研究
(In Vivo)

BMS-869780 (25 mg/kg; p.o.; 单次给药) 可在给药后 3 h 和 6 h 显著降低野生型 C57Bl/6 小鼠脑内 Aβ1-42 水平，但对脑内总 Aβ1-x 水平无显著影响[1]。

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

Animal Model: C57Bl/6 (12-week-old male/female, wild-type)[1]
Dosage: 25 mg/kg
Administration: p.o.; single dose
Result: Significantly decreased brain Aβ1-42 levels relative to vehicle controls at 3 hours post-dose.
Showed no significant change in brain Aβ1-x levels relative to vehicle controls at 3 hours post-dose.
Remained significantly decreased brain Aβ1-42 levels relative to vehicle controls at 6 hours post-dose.
Showed no significant change in brain Aβ1-x levels relative to vehicle controls at 6 hours post-dose.
Produced no significant synergistic reduction in brain Aβ1-x levels when administered in combination with GSM-2 at 3 or 6 hours post-dose.
Showed a small significant reduction in Aβ1-42 levels at 6 hours post-dose relative to BMS-869780 alone when administered in combination with GSM-2.
分子量

452.92

Formula

C23H22ClFN6O
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

BMS-869780 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

BMS-8697801235493-78-3BMS869780BMS 869780γ-secretaseAmyloid-βGamma secretaseβ-amyloid peptideAβAbetacell culturesAβ1-42Aβ1-xwild-type C57Bl/6 miceAβ1-40mouse modelshuman neuroglioma H4-APPsw cellsα-CTFamyloid-β peptideInhibitorinhibitorinhibit

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