EXP-3174, also known as Losartan Carboxylic Acid, is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver. EXP-3174 produced a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Effects of licochalcon A on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats.
Choi JS, et al. Pharmazie. 2013 Nov;68(11):882-8. PMID: 21709429.
Effects of HMG-CoA reductase inhibitors on the pharmacokinetics of losartan and its main metabolite EXP-3174 in rats: possible role of CYP3A4 and P-gp inhibition by HMG-CoA reductase inhibitors.
Yang SH, et al. Pharmacology. 2011;88(1-2):1-9. PMID: 21709429.
ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
ML-265 (TEPP-46) is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2).
LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase).
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