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D1464 | JW47

Molecular Formula C65H115N11O12
Molecular Weight 1357.9
Structure
Description a quinolinium cation tethered to cyclosporine

Toxicity Dose Time Species Model Method Action Positive criterion Reference
TRANSMEMBRANE POTENTIAL 40nM rat rat cortical neurons and isolated rat liver mitochondria mitochondrial membrane potential was measured in tetramethylrhodamine methyl ester (TMRM)-loaded neurons using ImageXpress MicroXL, and in rhodamine-123 loaded isolated mitochondria using a fluorescent plate reader Negative 324
TRANSMEMBRANE POTENTIAL 1 μM rat rat cortical neurons and isolated rat liver mitochondria mitochondrial membrane potential was measured in tetramethylrhodamine methyl ester (TMRM)-loaded neurons using ImageXpress MicroXL, and in rhodamine-123 loaded isolated mitochondria using a fluorescent plate reader 324
OPENING OF PERMEABILITY TRANSITION PORE (PTP) 10nM rat liver mitochondria Assess Ca2+-mediated PT pore formation by Calcium Retention Capacity Assay (Fluo-5N fluorescence was measured in the extramitochondrial solution following repeated additions of Ca2+) inhibit half-maximal inhibition 324
MITOCHONDRIAL PARAMETERS 200nM rat rat cortical neurons and isolated rat liver mitochondria oxygen consumption (Oroboros Oxygraph-2K) Negative 324
ATP SYNTHESIS 200nM rat rat cortical neurons and isolated rat liver mitochondria ATP production ( Cell Titer Glo reagent) Negative 324

Target Dose Time Species Model Method Action Positive criterion Reference
Peptidyl-prolyl cis-trans isomerase F, mitochondrial 504.5 ± 9.2 nM (CypA), 298.0 ± 17.9 nM( K133I CypD) Fluorescence Polarization Assay to measure affinity of ligands to cyclophilins (fluorescein-PEG-CsA ligand as the probe) bind Ki 324


  • [Gly-(1S,2R,E)-8-quinolinium-1-hydroxy-2-methyloct-4-ene]1 CsA