| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
hGSK-3β 12 nM (IC50)
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|---|---|
| ln Vitro |
SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampus neurons[2].
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| ln Vivo |
In transgenic mice expressing P301L tau, SAR502250 (1–100 mg/kg; a single dose) attenuates tau hyperphosphorylation in the cortex and spinal cord[2]. Following Aβ25-35 infusion, SAR502250 (10–30 mg/kg; po once daily for 7 weeks) ameliorates the cognitive deficit in transgenic APP(SW)/Tau(VLW) mice[2]. In the inter-response time (IRT) bin (49-96 s), SAR502250 (10-30 mg/kg; one po) considerably raises the percentage of lever presses together with a notable rise in the percentage of reinforced responses[2]. SAR502250 (30 mg/kg; intraperitoneally once daily for 28 days) improves the physical state of the mice's coat that is deteriorated due to prolonged stress[2]. SAR502250 (10–60 mg/kg; one po) reduces the hyperactivity that stimulants cause in mice[2].
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| Animal Protocol |
Animal/Disease Models: Female P301L human tau transgenic mice (three-month-old; 32 g )[2]
Doses: 1, 3, 10, 30, 100 mg/kg Route of Administration: A single po Experimental Results: Attenuated dose-dependently tau phosphorylation in the cortex and spinal cord, with ED50s of 12.5 and 11.5 mg/kg, respectively. |
| References |
[1]. Fukunaga K, et, al. 2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; a new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6933-7.
[2]. Griebel G, et, al. The selective GSK3 inhibitor, SAR502250, displays neuroprotective activity and attenuates behavioral impairments in models of neuropsychiatric symptoms of Alzheimer's disease in rodents. Sci Rep. 2019 Dec 2;9(1):18045. |
| Molecular Formula |
C19H18FN5O2
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|---|---|
| Molecular Weight |
367.38
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| CAS # |
503860-57-9
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| SMILES |
C1CO[C@@H](C2=CC=C(C=C2)F)CN1C1N(C(=O)C=C(C2C=CN=CN=2)N=1)C
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (272.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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