1. Immunology/Inflammation
    GPCR/G Protein
  2. FLAP
    Leukotriene Receptor
  3. Veliflapon

Veliflapon (Synonyms: BAY X 1005; DG-031)

Cat. No.: HY-14165 Purity: >99.0%
Handling Instructions

Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

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

Veliflapon Chemical Structure

Veliflapon Chemical Structure

CAS No. : 128253-31-6

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10 mM * 1 mL in DMSO USD 382 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 820 In-stock
Estimated Time of Arrival: December 31
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Description

Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor[1]. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4[2].

IC50 & Target[1][2]

LTB4

 

LTC4

 

In Vitro

Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC50s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC50 of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan[3].

In Vivo

Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis[4].
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test[4].
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED40 of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay[4].

Animal Model: Female apoE/LDLR-DKO mouse model[4]
Dosage: 18.8 mg/kg
Administration: Diet; per day during 16 weeks
Result: Inhibited atherogenesis.
Molecular Weight

361.43

Formula

C₂₃H₂₃NO₃

CAS No.

128253-31-6

SMILES

O=C(O)[[email protected]](C1CCCC1)C(C=C2)=CC=C2OCC3=NC4=CC=CC=C4C=C3

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
References

Purity: >99.0%

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Keywords:

VeliflaponBAY X 1005DG-031BAY X1005BAY X-1005DG031DG 031FLAPLeukotriene Receptor5-lipoxygenase-activating protein5-LO activating proteinorallyactiveleukotrienesB4C45-lipoxygenaseactivatingproteinarachidonicacidmetabolismatherogenesisInhibitorinhibitorinhibit

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Veliflapon
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