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| 产品编号 | RC10061 |
| 说明书 | |
| CAS号 | 1416435-96-5 |
| 分子式 | C32H42N4O4 |
| 分子量 | 546.70 |
| 作用靶点 | Protease Activated Receptor (PAR) |
| 作用通路 | GPCR/G Protein |
| 储存 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 溶解性 | DMSO: 31.25 mg/mL (57.16 mM),Sonication is recommended. Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. Please use it as soon as possible. |
| 描述 | GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM. |
| In vitro | GB-88 inhibits iCa2+ release induced in HT29 cells by trypsin, 2f-LIGRLO-NH2 and GB110 (PAR2 agonists).?And antagonism by GB-88 is agonist dependent |
| In vivo | GB-88 inhibits PAR2-induced acute inflammation in vivo.GB-88 is both orally active and anti-inflammatory in vivo, with specific antagonist activity against four structurally and mechanistically different PAR2 agonists (2f-LIGRLO-NH2, trypsin, SLIGRL-NH2 and GB110). |
