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HCH6-1

Cat No.:V32864 Purity: ≥98%
HCH6-1 is a potent competitive dipeptide antagonist of formyl peptide receptor 1 (FPR1).
HCH6-1
HCH6-1 Chemical Structure CAS No.: 1435265-06-7
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
HCH6-1 is a potent competitive dipeptide antagonist of formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release of human neutrophils specifically activated by fMLF (FPR1 agonist). In animal experiments, HCH6-1 has a protective effect on acute lung injury (ALI) and may be utilized to study inflammatory lung diseases involving FPR1.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
HCH6-1, with an IC50 of 0.32 μM, markedly reduced the production of superoxide anion in fMLF (FPR1 agonist)-activated neutrophils in a cell-impermeable cytochrome c reduction assay. HCH6-1, with an IC50 of 4.98±0.27 μM and 17.68±2.77 μM, respectively, has a slight inhibitory effect on neutrophils activated by WKYMVm (a FPR1/FPR2 dual agonist) and MMK1 (a FPR2 agonist) [1]. HCH6-1 has no cytotoxic effect on human neutrophils because it does not cause LDH release, not even at 30 μM. In cell-free systems, HCH6-1 has no effect on the levels of DPPH radicals, xanthine/xanthine oxidase superoxide anion, or either of these [1]. At an IC50 of 0.57 μM, HCH6-1 dramatically reduces the release of elastase from fMLF-activated neutrophils. Nevertheless, HCH6-1 inhibits elastase release at higher concentrations in WKYMVm or MMK1-triggered neutrophils (IC50 of 5.22±0.69 μM and 10.00±0.65 μM, respectively) [1].
ln Vivo
Cavity inflammation was not induced by HCH6-1 alone (intraperitoneal injection; 50 mg/kg; 1 hour before or 30 minutes after LPS nebulization). In the presence of LPS, pretreatment with HCH6-1 decreased inflammatory cell infiltration and lung structural deformation. In LPS-induced ALI mice, HCH6-1 post-treatment demonstrated an inhibitory effect on neutrophil accumulation and lung damage [1].
Animal Protocol
Animal/Disease Models: C57BL/6 mice (20-25 g, 7-8 weeks old) [1]
Doses: 50 mg/kg
Route of Administration: intraperitoneal (ip) injection; 50 mg/kg; 1 hour before LPS spray or after LPS spray 30 min
Experimental Results: Improved ALI in LPS-induced mice. HCH6-1-mediated reduction in neutrophil recruitment is a protective mechanism in ALI mice.
References

[1]. Dipeptide HCH6-1 inhibits neutrophil activation and protects against acute lung injury by blocking FPR1. Free Radic Biol Med. 2017 May;106:254-269.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H27N3O4
Molecular Weight
469.531687021255
Exact Mass
469.2
CAS #
1435265-06-7
PubChem CID
71697968
Appearance
White to off-white solid powder
Density
1.259±0.06 g/cm3(Predicted)
Boiling Point
790.8±60.0℃at 760 mmHg
LogP
3.8
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
10
Heavy Atom Count
35
Complexity
717
Defined Atom Stereocenter Count
2
SMILES
COC(=O)[C@@H](CC1=CC=CC=C1)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)NC(=O)C4=CC=CC=C4
InChi Key
MPFZAIDTRUPTSU-LOSJGSFVSA-N
InChi Code
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
Chemical Name
methyl (2R)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~532.45 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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