SML1680

Ex26

Name: Ex26
Brand: SIGMA

≥98% (HPLC)

别名:

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

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关于此项目

经验公式（希尔记法）:

C₂₈H₂₈ClFN₂O₃

化学文摘社编号:

1233332-37-0

分子量:

494.98

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

主要文件

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InChI key

YVHNBORUVLWCKF-UHFFFAOYSA-N

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 25 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

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.).

Ex26 is a peripherally-restricted biphenylcarboxamide derivative that acts as a highly potent and subtype-selective S1P1 antagonist.