| Identification | Back Directory | [Name]
1-(5'-((1-(4-chloro-3-methylphenyl)ethyl)amino)-2'-fluoro-3,5-dimethyl-[1,1'-biphenyl]-4-carboxamido)cyclopropane-1-carboxylic acid | [CAS]
1233332-37-0 | [Synonyms]
Ex 26
S1P1-IN-Ex26
Ex26 >=98% (HPLC)
S1P1 IN Ex26,S-1P1-IN-Ex26,S1P1INEx26
1-({5'-[1-(4-Chloro-3-methyl-phenyl)-ethylamino]-2'-fluoro-3,5-dimethyl-biphenyl-4-carbonyl}-amino)-cyclopropanecarboxylic acid
1-(5'-((1-(4-chloro-3-methylphenyl)ethyl)amino)-2'-fluoro-3,5-dimethyl-[1,1'-biphenyl]-4-carboxamido)cyclopropane-1-carboxylic acid
1-[[[5'-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2'-fluoro-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]amino]-cyclopropanecarboxylic acid
Cyclopropanecarboxylic acid, 1-[[[5'-[[1-(4-chloro-3-methylphenyl)ethyl]amino]-2'-fluoro-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]amino]- | [Molecular Formula]
C28H28ClFN2O3 | [MDL Number]
MFCD30537540 | [MOL File]
1233332-37-0.mol | [Molecular Weight]
494.98 |
| Hazard Information | Back Directory | [Uses]
1-?[[[5''-?[[1-?(4-?Chloro-?3-?methylphenyl)?ethyl]?amino]?-?2''-?fluoro-?3,?5-?dimethyl[1,?1''-?biphenyl]?-?4-?yl]?carbonyl]?amino]?-cyclopropanecarboxyl?ic Acid is a potent and selective S1P1 receptor antagonist. | [Biological Activity]
Ex26 is a peripherally-restricted biphenylcarboxamide derivative th at 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/kgi.p.) in lymph nodes and pulmonary edema (2 hr post 30 mg/kg i.p.) in miceleading 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/di.p.). | [in vivo]
Ex26 (i.p.; 3 mg/kg; once daily; 3 d) treatment disrupts S1P1 signaling inhibiting the lymphocyte and thymocyte egress[1].
Ex26 (i.p.; 30 mg/kg; once daily; 15 d) treatment alleviates experimental autoimmune encephalomyelitis by S1P1 antagonism[1]. | Animal Model: | Eight-week-old male C57Bl/6J mice[1] | | Dosage: | 3 mg/kg | | Administration: | Intraperitoneal injection; 3 mg/kg; once daily; 3 days | | Result: | Induced lymphocyte sequestration at low doses, possessing an ED50 of 0.06 mg/kg after 2 hours treatment. Led to significant retention of T and B cells within the lymph nodes and significant decreases in T and B cells within the spleen. |
| Animal Model: | Eight-week-old male C57Bl/6J mice induced with experimental autoimmune encephalomyelitis[1] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; 30 mg/kg; once daily; 15 days | | Result: | Inhibited both lymphocyte infiltration and destruction of the white matter in the spinal cord of mice euthanized at the end of the experiment. |
| [storage]
Store at -20°C |
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Energy Chemical
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Merck KGaA
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