CYM-5442
规格
| Cas Number | 1094042-01-9 |
| 规格或纯度 | Moligand™ |
| 级别 | Moligand™ |
| 包装 | 25mg |
产品信息
| 品牌 | 阿拉丁 |
| Action Type | 激动剂 |
| Mechanism Of Action | S1P 1 受体激动剂 |
| 溶解性 | Solubility (25°C) In vitro Ethanol: mg/mL |
| 简短描述 | S1P 受体调节剂 |
| 英文简短描述 | S1P Receptor Modulators |
| 过滤标签 | S1P1 receptor Agonist,LPL Receptor,GPCR/G Protein |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | CYM-5442 是一种强效的选择性<sub>S1P1</sub>激动剂，EC50 为 1.35 nM。 |
| 英文描述 |
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. |