Digoxin is a widely used compound for ventricular rate control in patients with atrial fibrillation (AF), despite a scarcity of randomised trial data.Digoxin treatment was associated with a significant increase in all-cause mortality, vascular death, and sudden death in patients with AF. This association was independent of other measured prognostic factors, and although residual confounding could account for these results, these data show the possibility of digoxin having these effects. A randomised trial of digoxin in treatment of AF patients with and without heart failure is needed.
|Cell lines||A549 cells|
|Preparation method||Cells were treated with various concentrations of digoxin for 24 h and seeded in transwell chambers (8-μm pore size, 6.5-mm diameter), which were or were not coated with Matrigel. The upper wells were filled with serum-free media and A549 cells (2×104 or 1×104 cells per well). The lower wells of the transwells contained the same media with 10% FBS and digoxin at various concentrations.|
|Incubation time||24 h|
|Animal models||Sprague Dawley Rats|
|Formulation||0.5% sodium carboxymethylcellulose|
|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.
|Source||Nature (2011). Figure 4. Digoxin|
|Cell Lines||Th17 cells|
|Incubation Time||6 d|
|Results||In vitro digoxin treatment of expanded mouse Th17 cells derived from immunized mice inhibited both IL-23R (Fig. 4a) and IL-17a expression without affecting IFN-γ expression (Fig. 4b).|
|Source||Nature (2011). Figure 1. Digoxin|
|Cell Lines||Drosophila S2 cell|
|Results||Inhibition of RORγ activity by digoxin was specific, as there was no effect on the transcriptional activity of VP16 or of the related nuclear hormone receptors RORα and DHR3|
Digoxin use and risk of mortality in hypertensive patients with atrial fibrillation.
Okin PM, et al. J Hypertens. 2015 Mar 19. PMID: 25799208.
Digoxin use in patients with atrial fibrillation and adverse cardiovascular outcomes: a retrospective analysis of the Rivaroxaban Once Daily Oral Direct Factor Xa Inhibition Compared with Vitamin K Antagonism for Prevention of Stroke and Embolism Trial in Atrial Fibrillation (ROCKET AF).
Washam JB, et al. Lancet. 2015 Mar 5. PMID: 25749644.
TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20±10 μM for MMP.
TAPI-0 is an inhibitor which blocks the maturation of cytokines, soluble cyokine receptors and other proteins that require the action of proteases.
A sulfhydryl reactive heterobifunctional crosslinking reagent. Widely used probe for introducing maleimides groups into biomolecules. A probe for thiol groups in proteins.
|6-Maleimidohexanoic acid N-hydroxysuccinimide ester
6-Maleimidohexanoic acid N-hydroxysuccinimide ester(ECMS) is a useful protective group in antibody drug conjugates.
BAY1436032 specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells.
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