AT-051/43421517
Based on 1 Customer Validation
AT-051/43421517 is a PGK1 activator with a Kd of 2.45 μM. AT-051/43421517 induces enhanced glycolytic metabolism and maintains TCA cycle activity, while inhibiting ROS production and Apoptosis. AT-051/43421517 reduces Aβ deposition and Tau hyperphosphorylation. AT-051/43421517 alleviates neuropathological damage in the brains of 3×Tg-AD mice. AT-051/43421517 improves cognitive impairment. AT-051/43421517 can be used for research on Alzheimer's disease and Parkinson's disease.
For research use only. We do not sell to patients.
- Purity : 99.71%
- CAS No.: 1241957-37-8
- Formula: C20H20N2O
- Molecular Weight:304.39
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PGK1 2.45 μM (Kd) |
In Vitro
AT-051/43421517 (0.78-200 μM) directly binds to the PGK1 protein with a KD value of 2.45 µM[1].
AT-051/43421517 (10 µM; 48 h) protects PC12 cells from Rotenone (HY-B1756)-induced cell death by increasing cell viability to 87.97%[2].
AT-051/43421517 (0.25-2 μM; 24 h) enhances AβO-induced PGK1 enzymatic activity in SH-SY5Y cells at concentrations of 0.25, 1, and 2 µM[1].
AT-051/43421517 (0.25-1 μM; 24 h) protects SH-SY5Y cells against AβO-induced impairment of cell viability at concentrations of 0.25 and 1 µM[1].
AT-051/43421517 (0.25-1 μM; 24 h) reduces AβO-induced apoptosis in SH-SY5Y cells by maintaining the Bcl-2/Bax ratio[1].
AT-051/43421517 (24 h) alleviates AβO-induced ROS accumulation in SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y
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Concentration:0.25-2 μM
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Incubation Time:24 h pre-treatment; 24 h co-incubation
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Result:Significantly enhanced enzymatic activity of PGK1 at concentrations of 0.25, 1, and 2 µM in AβO-induced SH-SY5Y cells.
Significantly increased PGK1 activity at 1 µM and 2 µM in SH-SY5Y cells not exposed to AβO.
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Cell Line:SH-SY5Y
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Concentration:0.25-1 μM
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Incubation Time:24 h pre-treatment; 24 h co-incubation
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Result:Significantly protected SH-SY5Y cells from the AβO-induced impairment of cell viability.
Had no significant effect on the viability of SH-SY5Y cells.
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Cell Line:SH-SY5Y
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Concentration:0.25-1 μM
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Incubation Time:24 h pre-treatment; 24 h co-incubation
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Result:Significantly prevented the AβO-induced decrease in the anti-apoptotic protein Bcl-2 and the increase in the pro-apoptotic protein Bax, thereby preserving the Bcl-2/Bax ratio.
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Cell Line:PC12 cells
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Concentration:10 µmol/L (primary bioassay with 4 µmol/L rotenone); 10 µmol/L (secondary bioassay alone)
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Incubation Time:48 h
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Result:Increased cell viability to 87.97% compared to the model group in the primary bioassay.
Did not show statistically significant improvement of PC12 cell viability in the secondary bioassay.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:3×Tg-AD mice (female, 10 months old, B6;129-Psen1tm1Mpm Tg(APPSwe, tauP301L)1Lfa/Mmjax on mixed C57BL/6JB6 and 129S1/SvImJ background)[1]
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Dosage:0.5-1 mg/kg
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Administration:i.p.; daily; 28 days
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Result:Rescued the deficit in spontaneous alternation in the Y-maze test.
Restored novel object exploration to levels comparable with WT mice in the NOR test.
Increased target quadrant time and platform crossings while reducing escape latency in the MWM test.
Dose-dependently increased the latency to levels observed in WT mice in the PAT.
Mitigated the accumulation of neurofibrillary tangles in the cortex.
Reduced Aβ1-42 accumulation in the cortex and hippocampus (DG, CA1, CA3) and reduced the amyloid plaque burden.
Reversed the upregulation of APP, PS1, and Aβ1-42 in cortical and hippocampal lysates.
Markedly attenuated neuronal loss in the cortex and hippocampus and significantly reduced the number of astrocytes, with no significant effect on microglial numbers.
Ameliorated morphological alterations, resulting in more visible nucleoli and reduced pyknosis.
Suppressed apoptosis in the hippocampus and cortex, as evidenced by a marked increase in Bcl-2 expression and a concomitant decrease in Bax expression.
Led to a significant increase in PGK1 activity in the hippocampus and cortex, without significantly altering total PGK1 protein levels or its expression specifically in neurons.
Chemical Information
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CAS No. 1241957-37-8
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Appearance Solid
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Molecular Weight 304.39
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Formula C20H20N2O
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Color Light yellow to yellow
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SMILES
CN(C)C(C=C1)=CC=C1/C=C/C2=C3C(C=CC=C3OC)=NC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (16.43 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (291 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2853 mL | 16.4263 mL | 32.8526 mL | 82.1315 mL |
| 5 mM | 0.6571 mL | 3.2853 mL | 6.5705 mL | 16.4263 mL | |
| 10 mM | 0.3285 mL | 1.6426 mL | 3.2853 mL | 8.2131 mL | |
| 15 mM | 0.2190 mL | 1.0951 mL | 2.1902 mL | 5.4754 mL |
AT-051/43421517 Related Classifications
HY-182811 Related Classifications
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Keywords
- AT-051/43421517
- 1241957-37-8
- Apoptosis
- Phosphoglycerate Kinase (PGK)
- Reactive Oxygen Species (ROS)
- Amyloid-β
- Tau Protein
- glycolytic metabolism enhancer
- PGK1
- apoptosis inhibitor
- ROS production
- tau hyperphosphorylation
- cognitive impairment
- TCA cycle activity
- astrocyte number reduction
- glycolytic flux
- Aβ deposition
- Inhibitor
- inhibitor
- inhibit