1-[[[5′-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2′-fluoro-3,5-dimethyl[1,1′-biphenyl]-4-yl]carbonyl]amino]-cyclopropanecarboxylic acid

产品名称：

1233332-37-0
Ex26
1-[[[5′-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2′-fluoro-3,5-dimethyl[1,1′-biphenyl]-4-yl]carbonyl]amino]-cyclopropanecarboxylic acid

产品介绍：

产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist (IC₅₀ = 0.93 nM against S1PR1 and >3.1 μM against S1PR2/3/4/5). Ex26 significantly elevates CpG-A-stimulated interferon (IFN) production in plasmacytoid dendritic cell culture (10 μM) and prevents S1P1 agonist-induced S1P1 receptor internalization and polyubiquitinylation in HEK cells (0.1-1,000 nM). Ex26 induces lymphocyte sequestration (ED₅₀ = 0.06 mg/kg, i.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in mice, leading to the inhibition of lymphocyte and thymocyte egress (0.1 mg/kg/hr continuously for 3 days after a loading dose of 3 mg/kg). Ex26 has been shown to ameliorate experimental autoimmune encephalomyelitis (EAE) in a mouse MS model and elevate CpG-A-stimulated serum IFN upregulation in mice in vivo (30 mg/kg/d, i.p.).

基本信息

经验(实验)分子式	C₂₈H₂₈ClFN₂O₃
分子量	494.98
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 25 mg/mL, clear
储存温度	2-8℃
SMILES string	ClC1=CC=C(C(C)NC2=CC=C(F)C(C3=CC(C)=C(C(NC4(CC4)C(O)=O)=O)C(C)=C3)=C2)C=C1C

安全信息

危险声明	H413
危险分类	Aquatic Chronic 4
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable