Azeliragon (Synonyms: TTP488; PF-04494700)

Name: Azeliragon
Brand: MedChemExpress
SKU: HY-50682
Rating: 5.0 (15 reviews)

Cat. No.: HY-50682 Purity: 99.75%: Data Sheet
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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 with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).

For research use only. We do not sell to patients.

CAS No. : 603148-36-3

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Azeliragon:

Azeliragon (Standard) Get quote

15 Publications Citing Use of MCE Azeliragon

In Vivo Efficacy Study

Cell Migration/Invasion Assay

Cell Proliferation/Viability Assay

IHC

Cell Imaging/Staining

: Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541. [Abstract]; Azeliragon (5 μM; 6 h) in neutrophils significantly restrained HMGB1-driven neutrophil migration.

: Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541. [Abstract]; Azeliragon (5 μM; 6 h) in neutrophils, representative immunofluorescence micrographs of NETs generation.

: Azeliragon purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Apr:139:156541. [Abstract]; Azeliragon (5 μM; 6 h) in neutrophils decreased the protein expression by MPO, PAD4 and CitH3 detected by western blot.

: Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59. [Abstract]; Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed anti-tumor activity.

: Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59. [Abstract]; Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed no antiproliferative effect in vivo. Immunohistochemical analysis of 4175/NSG tumors for proliferation (Ki67).

: Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59. [Abstract]; Azeliragon (TTP488; 1 mg/kg; IP; twice per week for 40 days) in 8-week-old female NSG mice showed reduced lung metastasis, with TTP488 affecting metastasis more potently at this dose. Immunohistochemical analysis of human CK7 to assess for metastasis in 4175/NSG mouse lung tissue.

: Azeliragon purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2023 Jul 13;9(1):59. [Abstract]; 4T-1 cells were tail-vein injected into BALBc mice, and mice were treated IP twice per week with 1 mg/kg Azeliragon (TTP488) or FPS-ZM1 (or vehicle (DMSO) control). Representative IVIS images at day 13 are shown from n = 11 per group. Mice treated with either TTP488 or FPS-ZM1 had significantly reduced tumor burden (p = <0.05) in the lungs at day 13 compared to the vehicle controltreated mice.

: Azeliragon purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2023 May 4;25(5):886-898. [Abstract]; Azeliragon (TTP488; 3 mg/kg/days; given four days after tumor implantation for a two-week period) improved the survival of ic GL261-bearing mice.

: Azeliragon purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2023 May 4;25(5):886-898. [Abstract]; Azeliragon (TTP488;500 ng/mL; 2, 4, 6 days) did not affect the growth of primary human malignant glioma cell lines in vitro.

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Biological Activity
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References
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Description

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 with mild Alzheimer’s disease (AD)^[1]. Azeliragon also can cross the blood-brain barrier (BBB)^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
SUM149PT	IC₅₀	5.292 μM Compound: Azeliragon	Cytotoxicity against human triple negative SUM149PT cells assessed as cell viability measured by MTS assay Cytotoxicity against human triple negative SUM149PT cells assessed as cell viability measured by MTS assay	[PMID: 34763082]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:	Purified T cells from RAGE-/- or WT B6 mice.
Concentration:	4 nM
Incubation Time:	16 hours
Result:	Inhibited of WT but not RAGE-/- T cells, and significantly reduced the level of IFN-γ.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Prediabetic NOD/LtJ (6-7 week old) mice, NOD mice with spontaneous diabetes, WT BALB/c mice (8-10 week old) and B6 mice with diabetes ^[3].
Dosage:	100 mcg/d
Administration:	Intraperitoneal injection; every day
Result:	Prolonged islet auto and allograft survival.

Clinical Trial

Molecular Weight

532.12

Formula

C₃₂H₃₈ClN₃O₂

CAS No.

603148-36-3

Appearance

Solid

Color

White to light yellow

SMILES

ClC1=CC=C(C=C1)OC2=CC=C(C=C2)N3C(CCCC)=NC(C(C=C4)=CC=C4OCCCN(CC)CC)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (93.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8793 mL	9.3964 mL	18.7928 mL
5 mM	0.3759 mL	1.8793 mL	3.7586 mL
10 mM	0.1879 mL	0.9396 mL	1.8793 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (274 KB) SDS (396 KB)

COA (247 KB) HNMR (413 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8793 mL	9.3964 mL	18.7928 mL	46.9819 mL
	5 mM	0.3759 mL	1.8793 mL	3.7586 mL	9.3964 mL
	10 mM	0.1879 mL	0.9396 mL	1.8793 mL	4.6982 mL
	15 mM	0.1253 mL	0.6264 mL	1.2529 mL	3.1321 mL
	20 mM	0.0940 mL	0.4698 mL	0.9396 mL	2.3491 mL
	25 mM	0.0752 mL	0.3759 mL	0.7517 mL	1.8793 mL
	30 mM	0.0626 mL	0.3132 mL	0.6264 mL	1.5661 mL
	40 mM	0.0470 mL	0.2349 mL	0.4698 mL	1.1745 mL
	50 mM	0.0376 mL	0.1879 mL	0.3759 mL	0.9396 mL
	60 mM	0.0313 mL	0.1566 mL	0.3132 mL	0.7830 mL
	80 mM	0.0235 mL	0.1175 mL	0.2349 mL	0.5873 mL

Azeliragon Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Azeliragon603148-36-3TTP488 PF-04494700TTP 488TTP-488PF04494700PF 04494700PF-04494700Amyloid-ββ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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Azeliragon (Synonyms: TTP488; PF-04494700)

Customer Review

Other Forms of Azeliragon:

Azeliragon Related Antibodies

15 Publications Citing Use of MCE Azeliragon

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•Related Screening Libraries:

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Purity & Documentation

References

Customer Review

Azeliragon Related Antibodies

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Complete Stock Solution Preparation Table

Azeliragon Related Classifications

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