880546-17-8
中文名称
化合物 T27708
英文名称
L-Phenylalaninamide, N-[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-5-yl]amino]carbonyl]glycyl-L-lysyl-N-(diphenylmethyl)-
CAS
880546-17-8
分子式
C51H56Cl2N8O4
分子量
915.95
MOL 文件
880546-17-8.mol
结构式
基本信息
中文别名
化合物 T27708
英文别名
K14585
K-14585
K 14585
L-Phenylalaninamide, N-[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-5-yl]amino]carbonyl]glycyl-L-lysyl-N-(diphenylmethyl)-
K-14585
K 14585
L-Phenylalaninamide, N-[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-5-yl]amino]carbonyl]glycyl-L-lysyl-N-(diphenylmethyl)-
物理化学性质
| 沸点 | 1115.5±65.0 °C(Predicted) |
| 密度 | 1.30±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 12.35±0.46(Predicted) |
应用领域
用途一
K-14585 is a proteinase-activated receptor 2 antagonist. Pretreatment with K-14585 inhibited PAR(2)-mediated p65 NFkappaB phosphorylation and NFkappaB-DNA binding. K-14585 inhibited SLIGKV-stimulated IL-8 production, but given alone increased IL-8. K-14585 antagonized PAR(2) competitively, resulting in inhibition of PAR(2)-mediated signalling and physiological responses both in vitro and in vivo. K-14585 could be useful in evaluating PAR(2)-mediated biological events and might lead to a new generation of therapeutically useful antagonists.
常见问题列表
概述
K-14585 是一种肽竞争性 PAR2 拮抗剂。K-14585 可抑制 PAR2 依赖性 IL-8 的产生、NF-κB 磷酸化和 p38 信号传导。K-14585 可降低 SLIGKV (PAR2 激动剂多肽) 诱导的原代人角质形成细胞中的 Ca2+ 动员。