Setipiprant (ACT-129968) 是一种具有口服活性的选择性 CRTH2 拮抗剂。
| Cas No. | 866460-33-5 |
| 别名 | 司替匹仑,ACT-129968; KYTH-105 |
| Canonical SMILES | O=C(O)CN1C2=C(CN(C(C3=C4C=CC=CC4=CC=C3)=O)CC2)C5=C1C=CC(F)=C5 |
| 分子式 | C24H19FN2O3 |
| 分子量 | 402.42 |
| 溶解度 | DMSO : ≥ 36 mg/mL (89.46 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.IC50 value: 6.0 nMTarget: PGD2in vitro: Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma. |
m.cnreagent.com