Synonyms: (S)-2-({3'-[(R)-1-(4-Chloro-3-methyl-phenyl)-ethylamino]-3,5-dimethyl-biphenyl-4-carbonyl}-amino)-propionic acid; N-[[3'-[[(1R)-1-(4-Chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]-L-alanine; NIBR 0213; NIBR0213
Molecular Formula: C27H29ClN2O3
Molecular Weight: 464.98
Linear Structural Formula: C27H29ClN2O3
MDL Number: MFCD25977008
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist that blocks S1P1-selective ligand AUY954-induced Ca2+ mobilization (IC50 = 2.5 nM using human S1P1-transfected HeLa cells; IC50 >10 muM with human S1P2, S1P3, or S1P4 transfectants) and S1P-induced GTPgammaS recruitment (IC50 = 2.0/2.3/8.5 nM using membrane from human/murine/rat S1P1-transfected CHO cells; IC50 >10 muM with membrane from human S1P5 transfectant). NIBR-0213 induces long-lasting peripheral blood lymphocyte reduction in rats (EDmax = 1 mg/kg, ED50 = 0.2 mg/kg; p.o.) and exhibits therapeutic efficacy (30 mg/kg p.o; BID) in experimental autoimmune encephalomyelitis (EAE), a murine model of multiple sclerosis (MS), with no adverse effects to the animals.