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SML2099

Sigma-Aldrich

NIBR-0213

≥98% (HPLC)

Synonyme(s) :

(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

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About This Item

Formule empirique (notation de Hill):
C27H29ClN2O3
Numéro CAS:
1233332-14-3
Poids moléculaire :
464.98
Numéro MDL:
MFCD25977008
Code UNSPSC :
51111800
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

−20°C

Chaîne SMILES 

C[C@@H](C(O)=O)NC(C1=C(C)C=C(C2=CC=CC(N[C@@H](C3=CC=C(Cl)C(C)=C3)C)=C2)C=C1C)=O

Application

NIBR-0213 may be used as a selective sphingosine-1-phosphate receptor 1 (S1P1) antagonist to assess S1P-mediated nuclear factor kappa B (NF-κB)-p65 nuclear translocation in human induced astrocytes.

Actions biochimiques/physiologiques

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 μM with human S1P2, S1P3, or S1P4 transfectants) and S1P-induced GTPγS recruitment (IC50 = 2.0/2.3/8.5 nM using membrane from human/murine/rat S1P1-transfected CHO cells; IC50 >10 μM 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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Emanuela Colombo et al.
Frontiers in immunology, 11, 635-635 (2020-04-24)
Multiple sclerosis (MS) is an inflammatory neurodegenerative disease of the central nervous system (CNS) with heterogeneous pathophysiology. In its progressive course oligodendrocyte and neuroaxonal damage is sustained by compartmentalized inflammation due to glial dysregulation. Siponimod (BAF312), a modulator of two
Jean Quancard et al.
Chemistry & biology, 19(9), 1142-1151 (2012-09-25)
Lymphocyte trafficking is critically regulated by the Sphingosine 1-phosphate receptor-1 (S1P(1)), a G protein-coupled receptor that has been highlighted as a promising therapeutic target in autoimmunity. Fingolimod (FTY720, Gilenya) is a S1P(1) receptor agonist that has recently been approved for
Marc Bigaud et al.
PloS one, 11(12), e0168252-e0168252 (2016-12-23)
Homeostasis of vascular barriers depends upon sphingosine 1-phosphate (S1P) signaling via the S1P1 receptor. Accordingly, S1P1 competitive antagonism is known to reduce vascular barrier integrity with still unclear pathophysiological consequences. This was explored in the present study using NIBR-0213, a
Victoria Fang et al.
Nature immunology, 18(1), 15-25 (2016-11-15)
The lymph node periphery is an important site for many immunological functions, from pathogen containment to the differentiation of helper T cells, yet the cues that position cells in this region are largely undefined. Here, through the use of a
Keisuke Yanagida et al.
Proceedings of the National Academy of Sciences of the United States of America, 114(17), 4531-4536 (2017-04-12)
The vasculature of the central nervous system (CNS) forms a selective barrier termed the blood-brain barrier (BBB). Disruption of the BBB may contribute to various CNS diseases. Conversely, the intact BBB restricts efficient penetration of CNS-targeted drugs. Here, we report
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