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  3. SAR502250

SAR502250 

Cat. No.: HY-137472 Purity: 99.90% ee.: 99.31%
Handling Instructions

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
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5000 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

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

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].

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.

503860-57-9

SMILES

O=C1C=C(C2=NC=NC=C2)N=C(N3C[[email protected]](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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (272.20 mM; Need ultrasonic)

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
10 mM 0.2722 mL 1.3610 mL 2.7220 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

SAR502250SAR 502250SAR-502250GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3GSK3GSK-3βantidepressantAlzheimer’sdiseaseADInhibitorinhibitorinhibit

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SAR502250
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