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

Azeliragon (Synonyms: TTP488; PF-04494700)

Cat. No.: HY-50682 Purity: 98.79%
Handling Instructions

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

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10 mM * 1  mL in DMSO USD 169 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
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100 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 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].

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].

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

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (93.96 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (5.64 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3 mg/mL (5.64 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (5.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.79%

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Keywords:

AzeliragonTTP488PF-04494700TTP 488TTP-488PF04494700PF 04494700Amyloid-ββ-amyloid peptideAbetaInhibitorinhibitorinhibit

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Azeliragon
Cat. No.:
HY-50682
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