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Ex26

Names

[ CAS No. ]:
1233332-37-0

[ Name ]:
Ex26

[Synonym ]:
MFCD30537540
1-{[(5'-{[1-(4-Chloro-3-methylphenyl)ethyl]amino}-2'-fluoro-3,5-dimethyl-4-biphenylyl)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]-
Ex26
1-[[[5'-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2'-fluoro-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]amino]-cyclopropanecarboxylic acid
1-[[[5′-[[1-(4-Chloro-3-methylphenyl)ethyl]amino]-2′-fluoro-3,5-dimethyl[1,1′-biphenyl]-4-yl]carbonyl]amino]cyclopropanecarboxylic acid

Biological Activity

[Description]:

Ex26 (S1P1-IN-Ex26) is a potent and selective Sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease

[Target]

IC50: 0.93 nM (S1P1)[1]


[In Vitro]

Ex26 (0-10 μM; 1 h) treatment shows excellent selectivity for S1P1 over other Sphingosine 1-phosphate receptors[1]. Cell Viability Assay[1] Cell Line: U2OS cells, and Chinese hamster ovary cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Confirmed a potent and selective antagonist of S1P1 (IC50=0.93 nM).

[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.

[References]

[1]. Stuart M Cahalan, et al. Sphingosine 1-phosphate receptor 1 (S1P(1)) upregulation and amelioration of experimental autoimmune encephalomyelitis by an S1P(1) antagonist. Mol Pharmacol. 2013 Feb;83(2):316-21.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
634.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H28ClFN2O3

[ Molecular Weight ]:
494.98

[ Flash Point ]:
337.4±31.5 °C

[ Exact Mass ]:
494.177246

[ LogP ]:
6.12

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.639

Related Compounds