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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-NIBR-0213
NIBR-0213

Chemical Structure : NIBR-0213

CAS No.: 1233332-14-3

NIBR-0213 (NIBR 0213, NIBR0213)

货号: PC-61179Not For Human Use, Lab Use Only.

NIBR-0213 is a potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

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5 mg ¥2280 In stock
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25 mg ¥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NIBR-0213 is a potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).
NIBR-0213 displays potent and comparable potency on human and rat S1P1 with IC50 of 2.0 and 2.3 nM in GTPγ35S assays, 3,000-fold selectivity against human S1P5.
NIBR-0213 inhibits FTY720-phosphate-induced S1P1 internalization at 1 uM, induces long-lasting reduction of peripheral blood lymphocyte counts, shows comparable therapeutic efficacy to Fingolimod in experimental autoimmune encephalomyelitis (EAE).

物理化学性质&存储条件

分子量 464.98
分子式 C27H29ClN2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[[3'-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]-L-alanine

参考文献

1. Quancard J, et al. Chem Biol. 2012 Sep 21;19(9):1142-51.

2. Bigaud M, et al. PLoS One. 2016 Dec 22;11(12):e0168252.

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