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Begacestat

Name: Begacestat
Brand: TargetMol
SKU: T14525
Price: 99 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14525Cas No. 769169-27-9

Alias WAY-210953, WAY210953, GSI-953, GSI953

Begacestat (GSI-953) is a potent and selective gamma-secretase inhibitor (γ-secretase) that inhibits Amyloid-beta production with nanomolar potency, selectively inhibits cleavage of APP in cellular level Notch cleavage assays, reverses situational memory deficits, and can be used to study Alzheimer's disease.

Begacestat

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Catalog No. T14525Alias WAY-210953, WAY210953, GSI-953, GSI953Cas No. 769169-27-9

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$99	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	Begacestat (GSI-953) is a potent and selective gamma-secretase inhibitor (γ-secretase) that inhibits Amyloid-beta production with nanomolar potency, selectively inhibits cleavage of APP in cellular level Notch cleavage assays, reverses situational memory deficits, and can be used to study Alzheimer's disease.
Targets&IC50	endogenous Aβ:3 nM, β-Amyloid (1-40):6 nM, β-Amyloid (1-42):10 nM, Notch cleavage:74 nM
In vitro	In CHO cells overexpressing human APP, Begacestat inhibited Aβ42 with an IC₅₀ of 10 nM and Aβ40 with an IC₅₀ of 6 nM after 16 hours of treatment. In HeLa cells, the IC₅₀ for endogenous Aβ inhibition was 3 nM. Begacestat has reduced potency against Notch signaling, with an IC₅₀ of 74 nM for Notch cleavage, indicating selectivity between Aβ and Notch inhibition[2].
In vivo	In Tg2576 transgenic mice, oral administration (p.o.) of Begacestat resulted in a significant reduction of brain Aβ levels at 3 hours post-dose. A single 10 mg/kg dose led to a 60% reduction in Aβ40 and a 54% reduction in Aβ42 in brain tissue. In Sprague-Dawley rats, a 30 mg/kg oral dose produced a 78% reduction in brain Aβ levels after 4 hours[2].
Synonyms	WAY-210953, WAY210953, GSI-953, GSI953

Chemical Properties

Molecular Weight	391.74
Formula	C₉H₈ClF₆NO₃S₂
Cas No.	769169-27-9
Smiles	C([C@H](NS(=O)(=O)C=1SC(Cl)=CC1)CO)(C(F)(F)F)C(F)(F)F
Relative Density.	1.642 g/cm3

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (102.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.11 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5527 mL	12.7636 mL	25.5271 mL	127.6357 mL
5 mM	0.5105 mL	2.5527 mL	5.1054 mL	25.5271 mL
10 mM	0.2553 mL	1.2764 mL	2.5527 mL	12.7636 mL
20 mM	0.1276 mL	0.6382 mL	1.2764 mL	6.3818 mL
50 mM	0.0511 mL	0.2553 mL	0.5105 mL	2.5527 mL
100 mM	0.0255 mL	0.1276 mL	0.2553 mL	1.2764 mL

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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