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.
Elamipretide, also known as MTP-131, is a cardiolipin peroxidase inhibitor and mitochondria-targeted peptide.
Hexacosanoic acid is a long-chain fatty acid related to various diseases such as adrenoleukodystrophy (ALD), adrenomyeloneuropathy (AMN) and atherosclerosis.
Corn oil, extracted from the germ of corn, can be used as a carrier for drug molecules and has anti-tumor activity.
Palosuran, also known as ACT-058362, is a Urotensin-II receptor antagonist with an IC50 of 3.6±0.2 nM.
Dithiothreitol (DTT) is the common name for a small-molecule redox reagent known as Cleland's reagent; as a reducing or "deprotecting" agent for thiolated DNA.
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