SML2099
NIBR-0213
≥98% (HPLC)
동의어(들):
(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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모든 사진(1)
About This Item
실험식(Hill 표기법):
C27H29ClN2O3
CAS Number:
Molecular Weight:
464.98
MDL number:
UNSPSC 코드:
51111800
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
−20°C
SMILES string
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
InChI
1S/C27H29ClN2O3/c1-15-11-20(9-10-24(15)28)18(4)29-23-8-6-7-21(14-23)22-12-16(2)25(17(3)13-22)26(31)30-19(5)27(32)33/h6-14,18-19,29H,1-5H3,(H,30,31)(H,32,33)/t18-,19+/m1/s1
InChI key
KYHUARFFBDLROH-MOPGFXCFSA-N
애플리케이션
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.
생화학적/생리학적 작용
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.
Orally active, potent and selective S1P1 antagonist with therapeutic efficacy in a murine model of multiple sclerosis (MS).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis.
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
Sofia Anastasiadou et al.
Experimental neurology, 279, 243-260 (2016-03-17)
Fingolimod (FTY720) is a new generation oral treatment for multiple sclerosis (MS). So far, FTY720 was mainly considered to target trafficking of immune cells but not brain cells such as neurons. Herein, we analyzed FTY720's potential to directly alter neuronal
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
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
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
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