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HCH6-1 

Cat. No.: HY-101283 Purity: 98.95%
Handling Instructions

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.

For research use only. We do not sell to patients.

HCH6-1 Chemical Structure

HCH6-1 Chemical Structure

CAS No. : 1435265-06-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 193 In-stock
Estimated Time of Arrival: December 31
5 mg USD 175 In-stock
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10 mg USD 275 In-stock
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50 mg USD 825 In-stock
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100 mg USD 1400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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 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].

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.
Molecular Weight

469.53

Formula

C₂₈H₂₇N₃O₄

CAS No.

1435265-06-7

SMILES

O=C(N[[email protected]](C(N[[email protected]@H](C(OC)=O)CC1=CC=CC=C1)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4

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
In Vitro: 

DMSO : 250 mg/mL (532.45 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

HCH6-1Othersinflammatorylung diseasesALIacute lung injuryFPR1antagonistpulmonarycell infiltrationInhibitorinhibitorinhibit

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HCH6-1
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