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^[1].

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.

480.51

C₂₅H₂₈N₄O₆

2135481-84-2

CC(N[C@H](COCC1=CC=CC=C1)C(NCCCNC(/C(C#N)=C/C2=CC(O)=C(C=C2)O)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu L, et al. Optimized synthesis of 5N-D and the exploration of its role as a promising anti-aging agent via AKR1B1 inhibition and PI3K/Akt/Nrf2 regulation. Bioorg Chem. 2025 Sep;164:108886.  [Content Brief]