Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE) with Kd of 12.7 nM for human recombinant sRAGE. While RAGE transports amyloid-β (Aβ) from plasma into the CNS, Azeliragon is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) and is currently under development as a treatment option to potentially slow the progression of mild Alzheimer’s disease (AD)[1]. Azeliragon also can cross the blood-brain barrier (BBB)[2].
体内研究
Furthermore, Azeliragon administered intraperitoneally at a dosage of 100 mcg/day, effectively reduces both syngeneic islet grafts and islet allografts in NOD and B6 mice. These mice models include NOD/LtJ mice with spontaneous diabetes receiving islets from young prediabetic NOD/LtJ mice, and diabetic B6 mice receiving islets from WT BALB/c mice, showcasing its potential in immunological applications beyond neurodegenerative disease[3].
体外研究
In experimental settings, Azeliragon (at a concentration of 4 nM for 16 hours) has been shown to inhibit the activation of wild type mouse (WT) T cells while not affecting RAGE-deficient mice (RAGE-/-). This treatment also significantly reduces the production of IFN-γ, indicating its potential impact on immune modulation in neurological contexts[3].
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