Azeliragon (TTP488) 是一种口服生物可利用的晚期糖基化终末产物 (RAGE) 受体抑制剂，正在开发中作为减缓轻度阿尔茨海默病 (AD) 患者疾病进展的潜在治疗方法。
| Cas No. | 603148-36-3 |
| 别名 | 阿齐瑞格; TTP488; PF-04494700 |
| Canonical SMILES | ClC1=CC=C(C=C1)OC2=CC=C(C=C2)N3C(CCCC)=NC(C(C=C4)=CC=C4OCCCN(CC)CC)=C3 |
| 分子式 | C32H38ClN3O2 |
| 分子量 | 532.12 |
| 溶解度 | DMSO : 50 mg/mL (93.96 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).Target: RAGEin vitro: TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 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.[1]in vivo: The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2] References:
[1]. Burstein AH, et al. Effect of TTP488 in patients with mild to moderate Alzheimer's disease. BMC Neurol. 2014 Jan 15;14:12.
[2]. Saito S, et al. New therapeutic approaches for Alzheimer's disease and cerebral amyloid angiopathy. Front Aging Neurosci. 2014 Oct 20;6:290.
[3]. Chen Y, et al. RAGE ligation affects T cell activation and controls T cell differentiation. J Immunol. 2008 Sep 15;181(6):4272-4278. |
