Firibastat (QGC001) is an orally active EC33 precursor drug. Firibastat is A first-in-class (first-in-class) brain aminopeptidase A (APA) inhibitor (Ki=200 nM) that selectively and specifically inhibits the conversion of cerebral angiotensin II to angiotensin III and lowers blood pressure in hypertensive rats.
|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.
|Solubility||Wate ≥ 20 mg/mL|
|Related Aminopeptidase Products|
LTA4H metalloenzyme inhibitor LYS006 is a selective oral agent in multiple Ph.II studies for the study of inflammatory diseases, including ulcerative colitis and NASH.
Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
CHR-2797 is an aminopeptidase inhibitor for LAP, PuSA and Aminopeptidase N with IC50 of 100 nM, 150 nM and 220 nM, respectively.
Ubenimex, also known as bestatin, is a competitive protease inhibitor.
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