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PF-06751979

Name: PF-06751979
Brand: TargetMol
SKU: T12429
Rating: 4.5 (1 reviews)

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Catalog No. T12429Cas No. 1818339-66-0

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

PF-06751979

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Catalog No. T12429Cas No. 1818339-66-0

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
25 mg	$1,230	10-14 weeks	10-14 weeks
50 mg	$1,610	10-14 weeks	10-14 weeks

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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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Product Introduction

Bioactivity

Description	PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
Targets&IC50	BACE2:194 nM , BACE1:7.3 nM
In vitro	PF-06751979 demonstrates enhanced selectivity for BACE2 (IC50=194 nM) with a 27-fold improvement compared to literature examples and various chemical series in the BACE1 program.
In vivo	PF-06751979 demonstrates excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases, including BACE2. Acute administration results in a robust, dose-responsive, and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40, with peak inhibition of over 77% at 3 hours. [1].

Chemical Properties

Molecular Weight	455.5
Formula	C₁₈H₁₉F₂N₅O₃S₂
Cas No.	1818339-66-0
Smiles	[H][C@]12CSC(N)=N[C@]1(CO[C@@H](C)C2)c1nc(NC(=O)c2ccc(OC(F)F)cn2)cs1
Relative Density.	1.66 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: 50 mg/mL (109.77 mM), Sonication is recommended.

DMSO: 150 mg/mL (329.31 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.24 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1954 mL	10.9769 mL	21.9539 mL	109.7695 mL
5 mM	0.4391 mL	2.1954 mL	4.3908 mL	21.9539 mL
10 mM	0.2195 mL	1.0977 mL	2.1954 mL	10.9769 mL
20 mM	0.1098 mL	0.5488 mL	1.0977 mL	5.4885 mL
50 mM	0.0439 mL	0.2195 mL	0.4391 mL	2.1954 mL
100 mM	0.0220 mL	0.1098 mL	0.2195 mL	1.0977 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