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
- 화학식: C23H22ClFN6O
- 분자량:452.92
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
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. Further protocols information, click here.
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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분자량 452.92
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
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Directly Induced Neuron Culture
Directly induced neuron culture converts somatic cells, most commonly fibroblasts, into induced neurons without passing through a pluripotent or neural progenitor stage; classic evidence shows that mouse fibroblasts can be converted by Ascl1, Brn2/Pou3f2, and Myt1l, human fibroblasts can be converted by defined neuronal transcription factors, and human fibroblasts can also be converted by miR-9/9-124 with neurogenic or subtype-specifying transcription factors. The readout is acquisition of neuronal identity and function, assessed by neuronal morphology, neuronal markers such as Tuj1/βIII-tubulin, MAP2, synapsin, and subtype markers when relevant, together with functional assays such as action-potential firing, synaptic activity, and electrophysiology.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)