A dual FLAP/sEH inhibitor
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Diflapolin

Item No. 28103

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(2-benzothiazolylmethoxy)-2-methylphenyl]-N'-(3,4-dichlorophenyl)-urea
CAS Number
724453-98-9
Molecular Formula
C22H17Cl2N3O2S
Formula Weight
458.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2.5mg/mLDMSO: 1.6mg/mL
λmax
259 nm
SMILES
CC1=C(NC(NC2=CC(Cl)=C(Cl)C=C2)=O)C=CC(OCC3=NC4=C(C=CC=C4)S3)=C1
InChi Code
InChI=1S/C22H17Cl2N3O2S/c1-13-10-15(29-12-21-26-19-4-2-3-5-20(19)30-21)7-9-18(13)27-22(28)25-14-6-8-16(23)17(24)11-14/h2-11H,12H2,1H3,(H2,25,27,28)
InChi Key
FGXLEECGXSDIMM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $52

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    5 mg

    $227

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    10 mg

    $396

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    Product Description

    Diflapolin is a dual inhibitor of 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH).1 It inhibits formation of the 5-lipoxygenase (5-LO) products leukotriene B4 (LTB4; Item No. 20110) and 5-HpETE (Item No. 44230) in isolated human monocytes and neutrophils (IC50s = 30 and 170 nM, respectively) and inhibits the epoxide hydrolase activity of sEH with an IC50 value of 20 nM in a cell-free assay. It is selective for FLAP and sEH over other arachidonic acid metabolism enzymes, including 5-LO, LTC4 synthase, mPGES-1, COX-1, or COX-2 in cell-free assays, as well as 12- and 15-LO in neutrophils. Diflapolin (1, 3, and 10 mg/kg) decreases inflammation in a mouse model of peritonitis induced by zymosan, reducing the production of LTB4 and LTC4 and inhibiting leukocyte recruitment.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Garscha, U., Romp, E., Pace, S., et al. Pharmacological profile and efficiency in vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase. Sci. Rep. 7(1), 9398 (2017).