[CAS NO. 1435265-06-7] HCH6-1
PRODUCTS SPECIFICATIONS [1435265-06-7]
DESCRIPTION [1435265-06-7]
Overview
| MDL | MFCD32197174 |
|---|---|
| Molecular Weight | 469.53 |
| Molecular Formula | C28H27N3O4 |
| SMILES | O=C(N[C@H](C(N[C@@H](C(OC)=O)CC1=CC=CC=C1)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4 |
1 Publications Citing Use of MCE
Summary
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] .
IC50 & Target
IC50: Formyl peptide receptor 1 (FPR1) [1]
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 IC
50
of 0.32 μM. HCH6-1 has fewer inhibitory effects in WKYMVm (dual FPR1/FPR2 agonist)- and MMK1 (FPR2 agonist)-activated neutrophils, with IC
50
s 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 IC
50
of 0.57 μM. However, in neutrophils triggered by WKYMVm or MMK1, HCH6-1 inhibits elastase release at higher concentrations, with IC
50
s of 5.22±0.69 μM and 10.00±0.65 μM, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6 mice (20-25 g, 7-8 weeks old) [1] |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; 50 mg/kg; 1 h before LPS spray or 30 min after LPS spray |
| Result: |
Ameliorated ALI in LPS-induced mice.
HCH6-1-mediated decreasing of neutrophil recruitment serves as a protective mechanism in ALI mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 532.45 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1298 mL | 10.6489 mL | 21.2979 mL |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution