Azeliragon (TTP488)

Synonyms: PF-04494700

Azeliragon (TTP488, PF-04494700) is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE), which is an immunoglobulin-like cell surface receptor overexpressed in brain tissues of patients with AD.

Azeliragon (TTP488) Chemical Structure

Azeliragon (TTP488) Chemical Structure

CAS No. 603148-36-3

Purity & Quality Control

Azeliragon (TTP488) Related Products

Biological Activity

Description Azeliragon (TTP488, PF-04494700) is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE), which is an immunoglobulin-like cell surface receptor overexpressed in brain tissues of patients with AD.
Targets
RAGE [1]
In Vivo
In vivo

Preclinical studies in animal models of alzheimer disease (tgAPPSwedish/London) have shown azeliragon to decrease Aβ plaque deposition; reduce total Aβ brain concentration while increasing plasma Aβ levels; decrease sAPPβ while increasing sAPPα; reduce levels of inflammatory cytokines; and slow cognitive decline and improve cerebral blood flow[1].

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00287183 Completed
Diabetic Nephropathy
Pfizer
February 2006 Phase 2

Chemical Information & Solubility

Molecular Weight 532.12 Formula

C32H38ClN3O2

CAS No. 603148-36-3 SDF --
Smiles CCCCC1=NC(=CN1C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C4=CC=C(C=C4)OCCCN(CC)CC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (187.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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