BMS-869780
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1235493-78-3
- 分子式: C23H22ClFN6O
- 分子量:452.92
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
BMS-869780 alone does not inhibit the production of total Aβ, but when combined with acidic GSMs (GSM-2 or GSM-1 (HY-119165)) in human glioma H4-APPsw cells, it exhibits strong synergistic inhibitory effects on the production of Aβ1-x and Aβ1-40 (with combination index values as low as 0.05-0.06), and can induce the accumulation of α-CTF[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (12-week-old male/female, wild-type)[1]
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Dosage:25 mg/kg
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Administration:p.o.; single dose
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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.
化学情報
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CAS 番号 1235493-78-3
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分子量 452.92
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分子式 C23H22ClFN6O
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SMILES
N(C=1N=C2[C@@H](CCCCN2N1)C3=CC=C(F)C=C3)C4=CC(OC)=C(C=C4)N5C=NC(Cl)=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)