CYM-5442 , CAS No.1094042-01-9, Agonist of S1P 1 receptor

Item Number

C412806

• Synonyms: CYM5442|1094042-01-9|CYM-5442|2-({4-[5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl}amino)ethan-1-ol|2-((4-(5-(3,4-Diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)amino)ethanol|2-[[4-[5-(3,4-diethoxyphenyl)-1,2,4-ox
• Specifications & Purity: Moligand™
• Biochemical and Physiological Mechanisms: CYM-5442 is a potent and selective S1P₁ agonist with EC50 of 1.35 nM.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: AGONIST
• Mechanism of action: Agonist of S1P 1 receptor

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.