An S1P5 agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006

A-971432 – 10 mg

Brand:
Cayman
CAS:
1240308-45-5
Storage:
-20
UN-No:
Non-Hazardous - /

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).{42320} 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 Huntington’s disease when administered at a dose of 0.1 mg/kg.{42320,42321} 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.{42320}  

 

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SKU: 25326 - 10 mg Category:

Description

An S1P5 agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively); inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM); increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model at 1 µM; attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s disease at 0.1 mg/kg; decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6/2 mice at 0.1 mg/kg; increases spontaneous alternation in the t-maze in aged mice at 0.1 mg/kg,

Formal name: 1-[[4-[(3,4-dichlorophenyl)methoxy]phenyl]methyl]-3-azetidinecarboxylic acid

Synonyms: 

Molecular weight: 366.2

CAS: 1240308-45-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

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