| CAS NO: | 1164462-05-8 |
| 包装 | 价格(元) |
| 10mM 1 mL in DMSO | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1164462-05-8 |
| 化学名 | (2E)-N-[2-(2-methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide |
| Canonical SMILES | COC1=CC(/C=C/C(NCCN2C(C)=CC3=C2C=CC=C3)=O)=CC(OC)=C1OC |
| 分子式 | C23H26N2O4 |
| 分子量 | 394.5 |
| 溶解度 | ≤5mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| 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 | IC50: 2.4 nM for KB EP2; 11.4 nM for KB EP4 TG4-155 is a brain penetrant EP2 antagonist. Prostaglandin E2 (PGE2) evokes distinct responses via four different ‘E prostanoid’ (EP) receptors. EP2, a G protein-coupled receptor, has diverse roles, such as those in cancer, inflammation, and neuroprotection. In vitro: Using a set of cell-based TR-FRET assays of cAMP formation, a previous study screened a small molecule library and identified TG4-155 and TG4-166 as the most potent ones. TG4-155 and TG4-166 also showed robust inhibition of PGE2 -induced cAMP accumulation in human EP2-overexpressing C6 glioma cells, without affecting prostaglandin EP4 or β2-adrenergic receptors. Both TG4-155 and TG4-166 could cause a robust rightward shift in the PGE2 dose–response curve without affecting the maximal response to PGE2. TG4-155 at 1 μM caused 1,120-fold shift and TG4-166 at 1 μM caused a 651-fold shift in the PGE2 EC50 [1]. In vivo: TG4-155 could significantly reduced neuronal injury in hippocampus when administered in mice beginning 1 h after termination of pilocarpine-induced status epilepticus. The salutary actions of TG4-155 raised the possibility that selective block of EP2 signaling through small molecules can be an innovative therapeutic strategy for inflammation-related brain injury [1]. Clinical trial: So far, no clinical study has been conducted. Reference: |
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