CYM-5442 - Moligand™ , Agonist of S1P 1 receptor, CAS No.1094042-01-9, Agonist of S1P 1 receptor
In stock
SKU
C412806
S1P Receptor Modulators
Information
CYM-5442 CYM-5442 is a potent and selective S1P 1 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.
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.
More Information
| CAS | 1094042-01-9 |
|---|---|
| Synonyms | DTXSID70648731 | 1-PIPERIDINEBUTANOL, .ALPHA.-(4-(1,1-DIMETHYLETHYL)PHENYL)-4-(HYDROXYDIPHENYLMETHYL)- | CHEBI:188539 | AS-16780 | Q27076958 | AKOS027250728 | N11214 | 2-((4-(5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)amino)eth |
| Specifications & Purity | Moligand™ |
| Storage | Store at -20°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | Information CYM-5442 CYM-5442 is a potent and selective S1P 1 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. 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. |
| Solubility | Solubility (25°C) In vitro Ethanol: mg/mL |
| Target | S1PR1 |
| PubChem CID | 25110406 |
| Molecular Formula | C23H27N3O4 |
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