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Ex26
产品别名
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C28H28ClFN2O3 |
| Molecular weight | 494.98 |
| NACRES | NA.77 |
| Biochem/physiol Actions【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.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 25 mg/mL, clear |
| storage temp.【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 |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Hazard Statements | H413 |
| Hazard Classifications【危险分类】 | Aquatic Chronic 4 |
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
