2. Neuronal Signaling
  3. Amyloid-β
  4. Azeliragon

Azeliragon  (Synonyms: TTP488; PF-04494700)

Cat. No.: HY-50682 Purity: 99.70%
COA Handling Instructions

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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 in patients 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.

Azeliragon Chemical Structure

Azeliragon Chemical Structure

CAS No. : 603148-36-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 70 In-stock
Solution
10 mM * 1 mL in DMSO USD 70 In-stock
Solid
1 mg USD 33 In-stock
5 mg USD 60 In-stock
10 mg USD 100 In-stock
50 mg USD 320 In-stock
100 mg USD 520 In-stock
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 9 publication(s) in Google Scholar

Azeliragon Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

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.

Azeliragon Related Antibodies

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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.70%

COA (247 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

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.

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
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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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