Azeliragon

Modify Date: 2024-01-02 10:59:22

Azeliragon Structure
Azeliragon structure
Common Name Azeliragon
CAS Number 603148-36-3 Molecular Weight 532.116
Density 1.1±0.1 g/cm3 Boiling Point 667.7±65.0 °C at 760 mmHg
Molecular Formula C32H38ClN3O2 Melting Point N/A
MSDS N/A Flash Point 357.6±34.3 °C

 Use of Azeliragon


TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).Target: RAGEin vitro: TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.[1]in vivo: The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2]

 Names

Name 1-Propanamine, 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]-N,N-diethyl
Synonym More Synonyms

 Azeliragon Biological Activity

Description TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).Target: RAGEin vitro: TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.[1]in vivo: The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2]
Related Catalog
References

[1]. Burstein AH, et al. Effect of TTP488 in patients with mild to moderate Alzheimer's disease. BMC Neurol. 2014 Jan 15;14:12.

[2]. Saito S, et al. New therapeutic approaches for Alzheimer's disease and cerebral amyloid angiopathy. Front Aging Neurosci. 2014 Oct 20;6:290.

[3]. Chen Y, et al. RAGE ligation affects T cell activation and controls T cell differentiation. J Immunol. 2008 Sep 15;181(6):4272-4278.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 667.7±65.0 °C at 760 mmHg
Molecular Formula C32H38ClN3O2
Molecular Weight 532.116
Flash Point 357.6±34.3 °C
Exact Mass 531.265259
PSA 39.52000
LogP 8.98
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.572
Storage condition 2~8°C

 Synthetic Route

~%

Azeliragon Structure

Azeliragon

CAS#:603148-36-3

Literature: Hari, Anitha Patent: US2008/249316 A1, 2008 ; Location in patent: Page/Page column 6 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

[3-(4-{2-butyl-1-[4-(4-chlorophenoxy)-phenyl]-1H-imidazole-4-yl}-phenoxy)-propyl]-diethyl-amine
1-Propanamine, 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]-N,N-diethyl-
3-(4-{2-Butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl}phenoxy)-N,N-diethyl-1-propanamine
3-(hydroxymethyl)phenylboronic acid pinacol ester
UNII:LPU25F15UQ
3-(4-{2-Butyl-1-[4-(4-chlorphenoxy)phenyl]-1H-imidazol-4-yl}phenoxy)-N,N-diethylpropan-1-amin
3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzyl alcohol
Azeliragon
[3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-methanol
[3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethylamine
3-(4-{2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl}phenoxy)-N,N-diethylpropan-1-amine
TTP488
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