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Azeliragon

Cat. No. M9483
Azeliragon Structure
Synonym:

TTP488; PF-04494700

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 60  USD60 In stock
10mg USD 100  USD100 In stock
50mg USD 320  USD320 In stock
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Quality Control & Documentation
Biological Activity

Azeliragon is a potent and orally active RAGE inhibitor.

Chemical Information
Molecular Weight 532.12
Formula C32H38ClN3O2
CAS Number 603148-36-3
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Burstein AH, et al. Clin Pharmacol D ruq Dev. Assessment of Azeliragon QTc Liability Through Integrated, Model-Based Concentration QTc Analysis.

[2] Burstein AH, et al. J Prev Alzheimers Dis. Development of Azeliragon, an Oral Small Molecule Antagonist of the Receptor for Advanced Glycation Endproducts, for the Potential Slowing of Loss of Cognition in Mild Alzheimer's Disease.

[3] Bongarzone S, et al. J Med Chem. Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective.

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Keywords: Azeliragon, TTP488; PF-04494700 supplier, inhibitors, activators


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