An agonist of S1P1 and S1P5 receptors (Kis = 0.626 and 0.574 nM

Ceralifimod – 1 mg

Brand:
Cayman
CAS:
891859-12-4
Storage:
-20
UN-No:
Non-Hazardous - /

Ceralifimod is an agonist of the sphingosine-1-phosphate (S1P) receptors S1P1 and S1P5 (Kis = 0.626 and 0.574 nM, respectively).{40578} It is selective for S1P1 and S1P5 over S1P2-4 (Kis = >5,450, >5,630, and 28.8 nM, respectively). Ceralifimod induces calcium influx in CHO-K1 cells overexpressing S1P1 (EC50 = 1 nM) and cAMP accumulation in CHO-K1 cells overexpressing S1P1 or S1P5 (EC50s = 0.027 and 0.33 nM, respectively). In vivo, ceralifimod (0.03 and 0.1 mg/kg) reduces paw edema in a rat model of collagen induced arthritis (CIA). It also delays disease onset and inhibits lymphocyte infiltration of the spinal cord in a rat model of experimental autoimmune encephalomyelitis (EAE) and prevents disease relapse in a non-obese diabetic mouse model of relapsing-remitting EAE.{41833}  

 

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Description

An agonist of S1P1 and S1P5 receptors (Kis = 0.626 and 0.574 nM, respectively); selective for S1P1 and S1P5 over S1P2-4 (Kis = >5,450, >5,630, and 28.8 nM, respectively); induces calcium influx in CHO-K1 cells overexpressing S1P1 (EC50 = 1 nM) and cAMP accumulation in CHO-K1 cells overexpressing S1P1 or S1P5 (EC50s = 0.027 and 0.33 nM, respectively); reduces paw edema in a rat model of CIA at 0.03 and 0.1 mg/kg; delays disease onset and inhibits lymphocyte infiltration of the spinal cord in a rat model of EAE; prevents disease relapse in a non-obese diabetic mouse model of relapsing-remitting EAE

Formal name: 1-[[3,4-dihydro-6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-2-naphthalenyl]methyl]-3-azetidinecarboxylic acid

Synonyms:  ONO-4641

Molecular weight: 435.6

CAS: 891859-12-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Neuroscience|Neurodegenerative Disorders

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