GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Related Lipoxygenase Products|
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively.
AKBA is an active triterpenoid compound from the extract of Boswellia serrata and Boswellia carteri Birdw, exerts anti-inflammatory therapeutic effects and noncompetitively inhibits 5-lipoxygenase, topoisomerase, and leukocyte elastase.
BHQ is a inhibitor of SERCA ATPase.
MK 886 is a potent 5-lipoxygenase activating protein inhibitor (FLAP) (IC50 = 44 nM).
Zileuton is an orally active 5-lipoxygenase (5-LOX) inhibitor that inhibits LTB4 synthesis with IC50 values of 0.56, 2.3 and 2.6 μM in dog, rat and human blood respectively.
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