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.
For research use only. We do not sell to patients.
- CAS No.: 2135481-84-2
- Formula: C25H28N4O6
- Molecular Weight:480.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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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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CAS No. 2135481-84-2
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Molecular Weight 480.51
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ALR2-IN-9 Related Classifications
HY-175862 Related Classifications
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