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Drug intelligence / Profile preview
A-971432
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A-971432 is an orally bioavailable, highly selective sphingosine-1-phosphate receptor 5 (S1PR5) agonist originally discovered by AbbVie. It exhibits high potency for S1PR5 (IC50 of approximately 6 nM) with significant selectivity over S1PR1 and S1PR3. S1PR5 is predominantly expressed in the central nervous system, particularly on oligodendrocytes and brain endothelial cells, as well as on natural killer cells. Preclinical studies have demonstrated that A-971432 promotes oligodendrocyte progenitor cell (OPC) differentiation and remyelination, preserves blood-brain barrier (BBB) integrity, and reverses age-related cognitive decline. It has been investigated as a potential therapeutic candidate for neurodegenerative and demyelinating disorders, including multiple sclerosis, Alzheimer's disease, and Huntington's disease.
- Other names
- 1-(4-((3,4-dichlorobenzyl)oxy)benzyl)azetidine-3-carboxylic acid1-[[4-[(3,4-dichlorophenyl)methoxy]phenyl]methyl]-3-azetidinecarboxylic acid
02
Targets
S1PR5 (Sphingosine-1-phosphate receptor 5)
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