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BI-1935

Protein target name:
EPHX2Mechanism of action:
InhibitorRecommended Concentration for use in cells:
10 nM
Probe Availability
Probe Information
In vitro validation
Potency:
IC507 nM
Potency assay:
biochemical h-sEH binding assayPDB ID for probe-target interaction (3D structure):
3OTQStructure-activity relationship:
yesPotency assay (off target):
Internal screen against hCYP epoxygenases 2J2/2C9/2C19 and IL-2: > 100-fold selectivity achieved (> 1μM for all)In cell validation
Potency in cells:
IC50< 1 nM
Potency assay (cells):
cellular Hep G2-DHET assayProbe Selectivity in Cell:
Off Target Screen - Panlabs panel: 61/67 < 20% Inhibition @ 10 μM, 5/67 < 80% Inhibition @ 10 μM, Thromboxane Synthase 96% inhibition @ 10 μM (IC50 = 0.132 μM)
In vivo validation
Organism:
RatDose:
1.2 mg/Kg IV3 mg/Kg PORoute of delivery:
OralIntravenousSystemic clearance:
2.9 ml/min/kgFraction of probe bound to plasma protein:
85 %Cmax:
3.6 uMTmax:
2.7 h