3BDO is a cell-permeable, orally bioavailable, non-toxic butyrolactone derivative that is shown to competitively bind FKBP1A (FK506-binding protein 1A, 12 kDa) in a reversible manner, and suppress autophagy via the mTOR pathway. 3BDO inhibits both LPS- and oxLDL-induced autophagy in HUVECs, increases TIA1 phosphorylation, and reduces autophagosomes number. It is reported to be brain permeant, and significantly decreases atherosclerosis development in apoE-/- mice (100 mg/kg, q.d., p.o.). 3BDO increases IDE and neprilysin levels, lowers amyloid-β deposition in an AβPP/PS1 transgenic mouse model of Alzheimer′s disease, and alleviates memory deficits. 3DBO protects the capability of Rheb1-deficient macrophages to perform phagocytosis. 3BDO also prevents the inhibitory effects of EX-527 on eukaryotic translation initiation factor-binding protein 1(4E-BP1) phosphorylation.
|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.
|Solubility||DMSO: ≥ 60 mg/mL|
An activator of mTOR inhibits oxLDL-induced autophagy and apoptosis in vascular endothelial cells and restricts atherosclerosis in apolipoprotein E⁻/⁻ mice.
Peng N, et al. Sci Rep. 2014 Jul 1;4:5519. PMID: 24980430.
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