CYM-5442

For research use only.

Catalog No.S2878

1 publication

CYM-5442 Chemical Structure

CAS No. 1094042-01-9

CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.

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Selleck's CYM-5442 has been cited by 1 publication

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Biological Activity

Description CYM-5442 is a potent and selective S1P1 agonist with EC50 of 1.35 nM.
In vitro

CYM-5442 is a chemically optimized version of an original hit (CYM-5181). CYM-5442 interacts with S1P1 in a binding pocket separate from key S1P1 residues Arg120 and Glu121 essential for high-affinity S1P binding and receptor activation. [1]

In vivo CYM-5442 is a full agonist for induction and maintenance of S1P1-dependent blood lymphopenia, decreasing B lymphocytes by 65% and T lymphocytes by 85% of vehicle. Induction of CYM-5442 lymphopenia is dose- and time-dependent, requiring serum concentrations in the 50 nM range. In addition, lymphopenia induced by CYM-5442 is reversed by W146 administration or upon pharmacokinetic agonist clearance. Pharmacokinetics in mice also indicates that CYM-5442 partitions significantly in central nervous tissue. [1]

Protocol

Animal Research:[1]
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  • Animal Models: Sprague-Dawley rats
  • Dosages: 1 mg/kg intravenous (i.v.) into the jugular or 2 mg/kg by oral gavage (p.o.).
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 409.48
Formula

C23H27N3O4

CAS No. 1094042-01-9
Storage powder
in solvent
Synonyms N/A

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