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Azeliragon (TTP488) RAGE Inhibitor

Name: Azeliragon (TTP488)
Brand: Selleck Chemicals
SKU: S6415
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S6415

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.

Chemical Structure

Molecular Weight: 532.12

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Quality Control

Batch: Purity: 99.81%

99.81

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other AGEs Inhibitors	Ipriflavone (Osteofix)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (187.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (11.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (11.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	532.12	Formula	C₃₂H₃₈ClN₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	603148-36-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PF-04494700			SMILES	CCCCC1=NC(=CN1C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C4=CC=C(C=C4)OCCCN(CC)CC

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	RAGE
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29616709/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-09)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07694089	NOT_YET_RECRUITING	High-grade Gliomas (HGG)	Akshitkumar MIstry	2026-10-01	PHASE2
NCT06831526	RECRUITING	Glioblastoma	Washington University School of Medicine	2025-11-06	EARLY_PHASE1
NCT07785856	NOT_YET_RECRUITING	T-dxd Resistant HER2-Positive; HER2 Low Metastatic Breast Cancer	The Methodist Hospital Research Institute	2026-12	PHASE1; PHASE2
NCT05789589	SUSPENDED	Cancer; Metastasis; Metastatic Cancer; Brain Metastases; Brain Metastases, Adult	Baptist Health South Florida	2023-11-17	PHASE1; PHASE2
NCT06724926	ACTIVE_NOT_RECRUITING	Solid Tumor; High-grade Glioma; Leptomeningeal Metastasis	NYU Langone Health	2025-02-18	PHASE1
NCT05256745	RECRUITING	Cancer Related Cognitive Decline; Non-metastatic Breast Cancer	Georgetown University	2023-06-06	PHASE1; PHASE2

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Handling Instructions

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