Azeliragon (also known as TTP488 and PF-04494700) is a potent and orally bioavailable RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.
理化性质和储存条件
| Molecular Weight (MW) | 532.12 |
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| Formula | C32H38ClN3O2 |
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| CAS No. | 603148-36-3 (free base); |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 10 mM |
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| Water: <1 mg/mL |
| Ethanol: N/A |
| SMILES Code | CCN(CC)CCCOC1=CC=C(C2=CN(C3=CC=C(OC4=CC=C(Cl)C=C4)C=C3)C(CCCC)=N2)C=C1 |
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| Synonyms | PF-04494700; PF 04494700; PF04494700; Azeliragon; TTP488; TTP-488; TTP 488; |
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实验参考方法
| In Vitro | In vitro activity: Azeliragon (also known as TTP488 and PF-04494700) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.
Cell Assay: Azeliragon is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of Azeliragon in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices. |
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| In Vivo | Azeliragon is administered i.p. daily at a dose of 100 mcg/d. Successful use of the RAGE inhibitor Azeliragon in Phase II testing has led to a Phase III clinical trial for AD patients. |
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| Animal model | N/A |
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| Formulation & Dosage | i.p. daily at a dose of 100 mcg/d |
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| References | BMC Neurol. 2014 Jan 15;14:12; Front Aging Neurosci. 2014 Oct 20;6:290. |
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