2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. SAR502250

SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).

For research use only. We do not sell to patients.

SAR502250 Chemical Structure

SAR502250 Chemical Structure

CAS No. : 503860-57-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Solid
1 mg USD 232 In-stock
5 mg USD 580 In-stock
10 mg USD 980 In-stock
25 mg USD 1900 In-stock
50 mg USD 3200 In-stock
100 mg USD 5000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

SAR502250 Related Antibodies

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GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2].

IC50 & Target[1]

hGSK-3β

12 nM (IC50)

In Vitro

SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SAR502250 Related Antibodies
In Vivo

SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau[2].
SAR502250 (10-30 mg/kg; p.o. once daily for 7 weeks) improves the cognitive deficit in transgenic APP(SW)/Tau(VLW) mice after infusion of Aβ25-35[2].
SAR502250 (10-30 mg/kg; a single p.o.) significantly increases the percentage of lever-presses in the inter-response time (IRT) bin (49-96 s), with a significant augmentation of the percentage of reinforced responses[2].
SAR502250 (30 mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat[2].
SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female P301L human tau transgenic mice (three-month-old; 32 g)[2]
Dosage: 1, 3, 10, 30, 100 mg/kg
Administration: A single p.o.
Result: Attenuated dose-dependently tau phosphorylation in the cortex and spinal cord, with ED50s of 12.5 and 11.5 mg/kg, respectively.
Molecular Weight

367.38

Formula

C19H18FN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(C2=NC=NC=C2)N=C(N3C[C@H](C4=CC=C(F)C=C4)OCC3)N1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (272.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7220 mL 13.6099 mL 27.2198 mL
5 mM 0.5444 mL 2.7220 mL 5.4440 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7220 mL 13.6099 mL 27.2198 mL 68.0494 mL
5 mM 0.5444 mL 2.7220 mL 5.4440 mL 13.6099 mL
10 mM 0.2722 mL 1.3610 mL 2.7220 mL 6.8049 mL
15 mM 0.1815 mL 0.9073 mL 1.8147 mL 4.5366 mL
20 mM 0.1361 mL 0.6805 mL 1.3610 mL 3.4025 mL
25 mM 0.1089 mL 0.5444 mL 1.0888 mL 2.7220 mL
30 mM 0.0907 mL 0.4537 mL 0.9073 mL 2.2683 mL
40 mM 0.0680 mL 0.3402 mL 0.6805 mL 1.7012 mL
50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3610 mL
60 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1342 mL
80 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8506 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
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SAR502250 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR502250503860-57-9SAR 502250SAR-502250GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3GSK3GSK-3βantidepressantAlzheimer’sdiseaseADInhibitorinhibitorinhibit

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