1-(5'-((1-(4-chloro-3-methylphenyl)ethyl)amino)-2'-fluoro-3,5-dimethyl-[1,1'-biphenyl]-4-carboxamido)cyclopropane-1-carboxylic acid Chemical Properties

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

powder

color 

white to beige

1-(5'-((1-(4-chloro-3-methylphenyl)ethyl)amino)-2'-fluoro-3,5-dimethyl-[1,1'-biphenyl]-4-carboxamido)cyclopropane-1-carboxylic acid Usage And Synthesis

Uses

1-?[[[5''-?[[1-?(4-?Chloro-?3-?methylphenyl)?ethyl]?amino]?-?2''-?fluoro-?3,?5-?dimethyl[1,?1''-?biphenyl]?-?4-?yl]?carbonyl]?amino]?-cyclopropanecarboxyl?ic Acid is a potent and selective S1P1 receptor antagonist.

Biological Activity

Ex26 is a peripherally-restricted biphenylcarboxamide derivative th at acts as a highly potent and subtype-selective S1P1 antagonist (IC50 = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). Ex26 significantly elevates CpG-A-stimulated interferon (IFN) production in plasmacytoid dendritic cell culture (10 μM) and prevents S1P1 agonist-induced S1P1 receptor internalization and polyubiquitinylation in HEK cells (0.1-1,000 nM). Ex26 induces lymphocyte sequestration (ED50 = 0.06 mg/kg, i.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in mice, leading to the inhibition of lymphocyte and thymocyte egress (0.1 mg/kg/hr continuously for 3 days after a loading dose of 3 mg/kg). Ex26 has been shown to ameliorate experimental autoimmune encephalomyelitis (EAE) in a mouse MS model and elevate CpG-A-stimulated serum IFN upregulation in mice in vivo (30 mg/kg/d, i.p.).

in vivo

storage

Store at +4°C