BMS 433796
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
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- CAS No.: 935525-13-6
- 화학식: C21H20F2N4O4
- 분자량:430.40
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
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gamma-secretase modulator 1Gamma-secretase Modulator
Biological Activity
제품 설명
IC50 & Target
γ-secretase[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.3 nM
Compound: BMS-433796
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Inhibition of gamma-secretase expressed in CHO cells expressing wild type human recombinant APP assessed as amyloid beta40 aggregation
Inhibition of gamma-secretase expressed in CHO cells expressing wild type human recombinant APP assessed as amyloid beta40 aggregation
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[PMID: 18556202] |
| H4 | IC50 |
0.3 nM
Compound: 40
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Inhibition of gamma secretase assessed as reduction of amyloid beta level in H4 cells
Inhibition of gamma secretase assessed as reduction of amyloid beta level in H4 cells
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[PMID: 17502137] |
| HEK293 | IC50 |
510 nM
Compound: BMS-433796
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Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
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[PMID: 17932033] |
| THP-1 | IC50 |
1.2 nM
Compound: BMS-433796
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Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
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[PMID: 17932033] |
| THP-1 | IC50 |
510 nM
Compound: BMS-433796
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Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
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[PMID: 17932033] |
In Vitro
BMS-433796 cause a concentration-dependent decrease in [3H]IN973 binding, with IC50 value of 1.2 nM, very similar to the IC50 values for inhibition of Aβ40 in human embryonic kidney cells overexpressing the Swedish mutation of APP of 0.8 nM, respectively, and for inhibition of Aβ42 of 0.4 nM, respectively[2].
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.
Chemical Information
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CAS No. 935525-13-6
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분자량 430.40
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화학식 C21H20F2N4O4
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SMILES
O[C@@H](C1=CC(F)=CC(F)=C1)C(N[C@@H](C)C(N[C@H]2C3=CC=CC=C3C=NN(C2=O)C)=O)=O
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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.
순도&문서
References
[1]. Prasad CV, et al. Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4006-11. [Content Brief]
[2]. Goldstein ME, et al. Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice. J Pharmacol Exp Ther. 2007 Oct;323(1):102-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS 433796 Related Classifications
HY-50884 Related Classifications
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