Cayman Reparixin

A-971432 is a sphingosine-1-phosphate receptor 5 (S1P₅) agonist that is selective for S1P₅ over S1P₁ and S1P₃ (IC₅₀s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P₅ (EC₅₀ = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntingtons disease when administered at a dose of 0.1 mg/kg.^, A-971432 (0.1 mg/kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6/2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg/kg.

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