| Identification | Back Directory | [Name]
Azeliragon | [CAS]
603148-36-3 | [Synonyms]
TTP488
TTP-488
CS-2071
TTP 488
CRL 40G
AZELIRAGON
PF04494700
PF-04494700
PF 04494700
PF-04494700,TTP488
Azeliragon (TTP488)
Azeliragon(PF-04494700,TTP488)
PF04494700;TTP-488;PF 04494700;TTP 488;PF-04494700;TTP488
3--4--2-Butyl-1--4--4-chlorphenoxy-phenyl--1H-imidazol-4-yl-phenoxy--N-N-diethylpropan-1-amin
3-(4-{2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine
3-(4-(2-butyl-1-(4-(4-chlorophenoxy)phenyl)-1H-imidazol-4-yl)phenoxy)-N,N-diethylpropan-1-amine
N-[3-[4-[2-Butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]propyl]-N,N-diethylamine
1-PropanaMine, 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-iMidazol-4-yl]phenoxy]-N,N-diethyl- | [EINECS(EC#)]
814-441-9 | [Molecular Formula]
C32H38ClN3O2 | [MDL Number]
MFCD11977600 | [MOL File]
603148-36-3.mol | [Molecular Weight]
532.12 |
| Chemical Properties | Back Directory | [Boiling point ]
667.7±65.0 °C(Predicted) | [density ]
1.11±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.33(Max Conc. mg/mL);94.58(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);9.4(Max Conc. mM)
DMF:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.62(Max Conc. mM)
Ethanol:50.5(Max Conc. mg/mL);94.9(Max Conc. mM) | [form ]
A crystalline solid | [pka]
10.16±0.25(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Azeliragon (TTP488, PF-04494700) is an orally bioavailable small molecule inhibitor that inhibits the receptor for advanced glycation end products (RAGE). RAGE is an immunoglobulin-like cell surface receptor that is overexpressed in the brains of Alzheimer's patients. | [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.
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| [target]
| Target | Value | RAGE
() | [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. DOI:10.1002/cpdd.689
[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. DOI:10.1021/acs.jmedchem.7b00058
[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. DOI:10.4049/jimmunol.181.6.4272 |
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Tags:603148-36-3
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