InformationCYM-5442 CYM-5442 is a potent and selective S1P 1 agonist with EC50 of 1.35 nM.In vitroCYM-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 vivoCYM-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.
Molecular Formula: C23H27N3O4
Molecular Weight: 409.48
PubChem CID: 25110406
Isomeric SMILES: CCOC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CCC(C4=CC=C3)NCCO)OCC
Related Documents: https://aladdin-for-icloud-store.oss-cn-hangzhou.aliyuncs.com/aladdinsci/pdp/sds/1/C412806-SCI_e2e839ed53e5c0e79e553d21b43c1891.pdf
- UPC:
- 12141723
- Condition:
- New
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- C412806-25mg
- CAS:
- 1094042-01-9
- Product Size:
- 25mg
- Precautionary Statement Codes:
- P264
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