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BMS-869780

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Catalog No. T218764 Copy Product Info
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BMS-869780 is an orally active non-acidic γ-secretase modulator. It can regulate the activity of γ-secretase, thereby altering the production profile of amyloid-beta peptides. BMS-869780 changes the relative levels of specific amyloid-beta peptide subtypes without reducing the overall production of amyloid-beta. Additionally, it acts synergistically with acidic γ-secretase modulators to inhibit the total production of amyloid-beta in cell cultures.

BMS-869780

Cas No. 1235493-78-3
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
BMS-869780 is an orally active non-acidic γ-secretase modulator. It can regulate the activity of γ-secretase, thereby altering the production profile of amyloid-beta peptides. BMS-869780 changes the relative levels of specific amyloid-beta peptide subtypes without reducing the overall production of amyloid-beta. Additionally, it acts synergistically with acidic γ-secretase modulators to inhibit the total production of amyloid-beta in cell cultures.
In vitro
BMS-869780 does not inhibit the production of total Aβ on its own; however, when used in combination with acidic GSM (GSM-2 or GSM-1) in human glioblastoma H4-APPsw cells, it exhibits a strong synergistic inhibitory effect on the production of Aβ1-x and Aβ1-40 (with a combination index as low as 0.05-0.06), and can induce the accumulation of α-CTF.
In vivo
Administered orally at a dose of 25 mg/kg, BMS-869780 significantly reduces brain levels of Aβ 1-42 in wild-type C57Bl/6 mice 3 and 6 hours post-treatment, with no significant effect on total brain Aβ 1-x levels.
Chemical Properties
Molecular Weight452.91
FormulaC23H22ClFN6O
Cas No.1235493-78-3
SmilesN(C=1N=C2[C@@H](CCCCN2N1)C3=CC=C(F)C=C3)C4=CC(OC)=C(C=C4)N5C=NC(Cl)=C5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: BMS-869780 in vivo | BMS-869780 in vitro | BMS-869780 formula | BMS-869780 molecular weight