For research use only. Not for therapeutic Use.
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases[1].
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[1].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[1].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[1].
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[1].
| CAS Number | 1435265-06-7 |
| Synonyms | methyl (2R)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate |
| Molecular Formula | C28H27N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H27N3O4/c1-35-28(34)25(16-19-10-4-2-5-11-19)31-27(33)24(30-26(32)20-12-6-3-7-13-20)17-21-18-29-23-15-9-8-14-22(21)23/h2-15,18,24-25,29H,16-17H2,1H3,(H,30,32)(H,31,33)/t24-,25+/m0/s1 |
| InChIKey | MPFZAIDTRUPTSU-LOSJGSFVSA-N |
| SMILES | COC(=O)C(CC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C4=CC=CC=C4 |
| Reference | [1]. Yang SC, et al. Dipeptide HCH6-1 inhibits neutrophil activation and protects against acute lung injury by blocking FPR1. Free Radic Biol Med. 2017 May;106:254-269 |
