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HIT105873687
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HIT105873687
  • HIT ID:HIT105873687
  • Cas No:1240308-45-5
  • 常用名:A-971432
  • IUPAC:1-({4-[(3,4-dichlorophenyl)methoxy]phenyl}methyl)azetidine-3-carboxylic acid
    IUPAC:1-({4-[(3,4-dichlorophenyl)methoxy]phenyl}methyl)azetidine-3-carboxylic acid
  • InChI key:WAAWETUDFSIYSD-UHFFFAOYSA-N
  • 分子式:C18H17Cl2NO3
  • 分子量:366.24
  • 氢键供体数 (HBD):1
  • 氢键受体数 (HBA):4
  • LogP:2.66
  • SMILES:OC(=O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1
    SMILES:OC(=O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1
  • 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 &#181M, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 &#181M) 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 Huntington’s disease when administered at a dose of 0.1 mg/kg.[1] [2] 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.[1]
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