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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- CAS No.: 1235493-78-3
- Formule: C23H22ClFN6O
- Masse moléculaire:452.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 1235493-78-3
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Masse moléculaire 452.92
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-869780 Related Classifications
HY-18326 Related Classifications
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