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SAR502250

Name: SAR502250
Brand: TargetMol
SKU: T35560
Rating: 4.5 (1 reviews)

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Catalog No. T35560Cas No. 503860-57-9

SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM, exhibiting antidepressant-like activity and being researched for potential application in Alzheimer's disease (AD) treatment.

SAR502250

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Catalog No. T35560Cas No. 503860-57-9

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,970	8-10 weeks	8-10 weeks
50 mg	$2,580	8-10 weeks	8-10 weeks
100 mg	$3,400	8-10 weeks	8-10 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	SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM, exhibiting antidepressant-like activity and being researched for potential application in Alzheimer's disease (AD) treatment.
Targets&IC50	GSK-3β (human):12 nM (IC50)
In vitro	SAR502250 (0.01-1 μM; 36 h) mitigates Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2].
In vivo	SAR502250, administered in varying dosages and methods, exhibits several notable effects in transgenic mice: it attenuates tau hyperphosphorylation in the cortex and spinal cord (1-100 mg/kg, single p.o.), improves cognitive deficits post-Aβ25-35 infusion (10-30 mg/kg, p.o. once daily for 7 weeks) in APP(SW)/Tau(VLW) mice, increases lever-presses in the IRT bin (49-96s) and reinforced responses (10-30 mg/kg, single p.o.), ameliorates chronic stress-induced coat degradation (30 mg/kg, i.p. once daily for 28 days), and decreases psychostimulant-induced hyperactivity (10-60 mg/kg, single p.o.)[2].

Chemical Properties

Molecular Weight	367.38
Formula	C₁₉H₁₈FN₅O₂
Cas No.	503860-57-9
Smiles	Cn1c(nc(cc1=O)-c1ccncn1)N1CCO[C@H](C1)c1ccc(F)cc1
Relative Density.	1.38 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

DMSO: 100 mg/mL (272.2 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (8.98 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	2.7220 mL	13.6099 mL	27.2198 mL	136.0989 mL
5 mM	0.5444 mL	2.7220 mL	5.4440 mL	27.2198 mL
10 mM	0.2722 mL	1.3610 mL	2.7220 mL	13.6099 mL
20 mM	0.1361 mL	0.6805 mL	1.3610 mL	6.8049 mL
50 mM	0.0544 mL	0.2722 mL	0.5444 mL	2.7220 mL
100 mM	0.0272 mL	0.1361 mL	0.2722 mL	1.3610 mL

Calculator

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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