ALR2-IN-9
ALR2-IN-9 is a potent ALR2 inhibitor (IC50 = 21.8 nM) with excellent antioxidant activity (EC50 for DPPH radical scavenging = 2.8 μM). ALR2-IN-9 interacts directly with Reactive Oxygen Species (ROS)/Reactive Nitrogen Species (RNS) and interrupts the free radical chain reactions, and as an endogenous enzymatic antioxidant regulator, which regulates enzyme functions of CAT and SOD. ALR2-IN-9 regulates PI3K/Akt/Nrf2 pathway to attenuate hyperglycemia-mediated mitochondrial superoxide overproduction in vitro, and ameliorates CuSO4- and H2O2-induced oxidative stress in vivo. ALR2-IN-9 prolongs lifespan of C. elegans via the regulation of stress response genes such as PMK-1. ALR2-IN-9 is a promising anti-aging drug candidate. ALR2-IN-9 can be used for diabetic complication research.
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- No. CAS: 2135481-84-2
- Fòrmula: C25H28N4O6
- Peso molecular:480.51
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Actividad biológica
Descripciòn
In Vitro
ALR2-IN-9 (compound 5N-D) (2.5-10 μM, 24h) ameliorates the impairments and ROS level in hyperglycemia Human Lymphatic Endothelial Cells (HLECs)[1].
ALR2-IN-9 (10 μM, 24 h) protects HLECs from high glucose-induced injury by activating the PI3K/Akt pathway, and reverses the hyperglycemia-reduced gene levels of Nrf2, HO-1, and NQO-1[1].
ALR2-IN-9 (10 μM, 1 h) demonstrates potent anti-oxidative efficacy by significantly attenuating the CuSO4-induced increase in ROS levels in zebrafish larvae[1].
ALR2-IN-9 (0.2 and 0.4 % wt%, 8 days) increases the mean lifespan, elevates the activity of SOD and CAT, and decreases the MDA level in C. elegans under oxidative stress[1].
ALR2-IN-9 (0.4 % wt%, 8 days) decreases ROS levels, reverses the H2O2-mediated suppression of AKT-1, SIR-2.1, DAF-16, and AGE-1, and further enhances the H2O2-induced upregulation of SKN-1 and PMK-1 in C. elegans[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HLECs
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Concentration:2.5, 5.0, and 10 μM
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Incubation Time:24 h
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Result:Reversed this hyperglycemia-induced impairments, restoring cell viability to 85.2 % at the dose of 10 μM.
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Cell Line:HLECs
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly increased the P-PI3K/PI3K and P-Akt/Akt ratios, compared to the high glucose group.
Failed to activate both PI3K and Akt in the presence of the specific PI3K inhibitor LY294002 (HY-10108).
Chemical Information
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No. CAS 2135481-84-2
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Peso molecular 480.51
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Fòrmula C25H28N4O6
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SMILES
CC(N[C@H](COCC1=CC=CC=C1)C(NCCCNC(/C(C#N)=C/C2=CC(O)=C(C=C2)O)=O)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ALR2-IN-9 Related Classifications
HY-175862 Related Classifications
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Keywords
- ALR2-IN-9
- 2135481-84-2
- Free Radical Scavengers
- Aldose Reductase
- Reactive Oxygen Species (ROS)
- PI3K
- Akt
- SOD
- p38 MAPK
- Keap1-Nrf2
- AKR1B1
- Aldo-keto reductase family 1 member B
- Phosphoinositide 3-kinase
- PKB
- Protein kinase B
- Superoxide Dismutase
- ALR2
- antioxidant
- ROS
- RNS
- free radical chain reactions
- PI3K/Akt/Nrf2 pathway
- lifespan
- stress response genes
- HLECs
- C. elegans
- PMK-1
- CAT
- oxidative stress
- Inhibitor
- inhibitor
- inhibit