AC55541
| CAS号 | 916170-19-9 | 货号 | BCP10730 |
| 中文名 | AC55541 | ||
| 英文名 | AC55541 | ||
| 中文别名 | |||
| 英文别名 | AC 55541;AC-55541; | ||
| 分子式 | C25H20BrN5O3 | 分子量 | 518.36 |
| 生物活性 | AC 55541 is a potent agonist of PAR2 with pEC50 value of 6.7 and functions range from 200 to 1000 nM .Protease-activated receptor 2 (PAR2) is a member of the large family of 7-transmembrane receptors and plays an important role in modulating inflammatory responses and acting as a sensor for proteolytic enzymes generated during infection. AC 55541 is a selective PAR2 agonist and has no effect on PAR1. Using a cellular proliferation assay (R-SAT), it showed that AC 55541 stimulated NIH-3T3 cells proliferation by activating PAR2 and receptor with F240S mutation constitutively active in all functional assays which nearly 30-fold sensitive to AC 55541 than SLIGRL and 2-furorl LIGRLO. When tested with human corneal epithelial (HCE) cells, administration of AC 55541 significantly induced the expression of PAR2 and inhibited Acanthamoeba plasminogen activator (aPA). In male Sprague-Dawley rat model with acute thermal nociception and edema in paw induced by SLIGRL-NH2 or trypsin, intrapaw administration of AC 55541 induced hind paw edema and thermal hyperalgesia at the doses as low as 30 ng and | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | PAR | ||
结构式
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