1. Immunology/Inflammation
    Metabolic Enzyme/Protease
  2. FLAP
    Epoxide Hydrolase
  3. Diflapolin

Diflapolin 

Cat. No.: HY-128171 Purity: 99.42%
Handling Instructions

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of  30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM).

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

Diflapolin Chemical Structure

Diflapolin Chemical Structure

CAS No. : 724453-98-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 81 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of  30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM)[1].

In Vivo

Diflapolin (1-10 mg/kg; i.p.; 30 min before zymosan injection) exhibits potent anti-inflammatory properties in in-vivo experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice (zymosan-induced peritonitis mouse model)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: I.p.; 30 min before zymosan injection
Result: Induced a significant reduction of LTC4 and LTB4 peritoneal levels, starting from the dose of 1 mg/kg and comparable to the effect of MK886.
Molecular Weight

458.36

Formula

C₂₂H₁₇Cl₂N₃O₂S

CAS No.

724453-98-9

SMILES

O=C(NC1=CC=C(Cl)C(Cl)=C1)NC2=CC=C(OCC3=NC4=CC=CC=C4S3)C=C2C

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 : 83.33 mg/mL (181.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1817 mL 10.9085 mL 21.8169 mL
5 mM 0.4363 mL 2.1817 mL 4.3634 mL
10 mM 0.2182 mL 1.0908 mL 2.1817 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.54 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

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

DiflapolinFLAPEpoxide Hydrolase5-lipoxygenase-activating protein5-LO activating proteinvascularpermeabilitycysteinyl-LTsneutrophilinfiltrationinflammationdiseasesInhibitorinhibitorinhibit

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Diflapolin
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