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CAS No. : 1435265-06-7
MCE 国际站:HCH6-1
产品活性:HCH6-1 是一种有效的甲酰肽受体 1 (FPR1) 的竞争性二肽拮抗剂。HCH6-1 抑制 fMLF (FPR1激动剂) 特异性激活的人中性粒细胞的趋化性、超氧阴离子生成和弹性酶释放。动物实验中,HCH6-1 对急性肺损伤 (ALI) 具有保护作用,可用于 FPR1 参与的炎症性肺部疾病的研究。
研究领域:GPCR/G Protein
作用靶点:Formyl Peptide Receptor (FPR)
In Vitro: In a cell-impermeable cytochrome c reduction assay, HCH6-1 significantly inhibits superoxide anion generation in fMLF (FPR1 agonist)-activated neutrophils with an IC50 of 0.32 μM. HCH6-1 has fewer inhibitory effects in WKYMVm (dual FPR1/FPR2 agonist)- and MMK1 (FPR2 agonist)-activated neutrophils, with IC50s of 4.98±0.27 μM and 17.68±2.77 μM, respectively.HCH6-1 does not induce LDH release even at 30 μM, so it does not have cytotoxic effects in human neutrophils. HCH6-1 does not alter the level of xanthine/xanthine oxidase superoxide anion and DPPH radical in cell-free systems.HCH6-1 significantly inhibits elastase release in fMLF-activated neutrophils, with an IC50 of 0.57 μM. However, in neutrophils triggered by WKYMVm or MMK1, HCH6-1 inhibits elastase release at higher concentrations, with IC50s of 5.22±0.69 μM and 10.00±0.65 μM, respectively.
In Vivo: HCH6-1 (intraperitoneal injection; 50 mg/kg; 1 h before LPS spray or 30 min after LPS spray) alone does not induce airspace inflammation. HCH6-1 pretreatment reduces inflammatory cell infiltration and distortion of pulmonary architecture in the presence of LPS. HCH6-1 posttreatment shows inhibitory effects on neutrophil accumulation and lung damage in LPS-induced ALI mice.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Targeted Diversity Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | BMS-986235 | MMK1 | {Boc}-Phe-Leu-Phe-Leu-Phe | FPR Agonist 43 | N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA | Ac9-25 TFA | WKYMVM TFA | WRW4 | FPR-A14 | Boc-MLF TFA | AG-09/1 | N-Formyl-Met-Leu-Phe-Lys | N-Boc-Phe-Leu-Phe-Leu-Phe | WKYMVM-NH2 TFA | ACT-389949 | Cyclosporin H
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