Azeliragon_product_DataBase

Bioactivity

Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD)[1]. Azeliragon also can cross the blood-brain barrier (BBB)[2].

Invitro

Azeliragon (4 nM; 16 hours; T cells) treatment inhibits of wild type mice (WT) but not the deletion of the receptor (RAGE-/- mice) T cells and significant reduction in the production of IFN-γ[3]. Cell Viability Assay[3] Cell Line:

In Vivo

Azeliragon (100 mcg/d; intraperitoneal injection; every day) treatment reduces syngeneic islet graft and islet allograft in NOD and B6 mice (Islets were isolated from young prediabetic NOD/LtJ mice and transplanted into NOD mice with spontaneous diabetes; islets were isolated from WT BALB/c mice and transplanted into B6 mice with diabetes)[3]. Animal Model:

Name

Azeliragon

CAS

603148-36-3

Formula

C32H38ClN3O2

Molar Mass

532.12

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Burstein AH, et al. Assessment of Azeliragon QTc Liability Through Integrated, Model-Based Concentration QTc Analysis. Clin Pharmacol Drug Dev. 2019 May;8(4):426-435. [2]. Bongarzone S, et al. Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective. J Med Chem. 2017 Sep 14;60(17):7213-7232. [3]. Chen Y, et al. RAGE ligation affects T cell activation and controls T cell differentiation. J Immunol. 2008 Sep 15;181(6):4272-8.

PeptideDB

Azeliragon

CAS: 603148-36-3 F: C32H38ClN3O2 W: 532.12