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SAR502250

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SAR502250

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.

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.

Pack Size	Price	Availability
25 mg	$1,970	8-10 weeks
50 mg	$2,580	8-10 weeks
100 mg	$3,400	8-10 weeks

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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

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 100 mg/mL (272.20 mM), Sonication is recommended.

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

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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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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

Keywords

SAR 502250SAR-502250SAR502250