t6541  (TargetMol)

Journal: Cell Reports Medicine

Article Title: Use of Patient Health Records to Quantify Drug-Related Pro-arrhythmic Risk

doi: 10.1016/j.xcrm.2020.100076

Figure Lengend Snippet:

Article Snippet: IBUTILIDE , TargetMol , T6541; CAS 122647-32-9.

Techniques: Recombinant, Software

Journal: Molecular pharmacology

Article Title: A High-Throughput Screening Assay to Identify Drugs that Can Treat Long QT Syndrome Caused by Trafficking-Deficient K V 11.1 (hERG) Variants.

doi: 10.1124/molpharm.121.000421

Figure Lengend Snippet: Fig. 8. Optimized Tl1 flux assay detected increased KV11.1-G601S-G965*X trafficking with three known KV11.1 inhibitors. (A) Bar graph show- ing Tl1 flux Z scores after 24-hour treatment with E-4031. 56 wells were selected from central rows of the plate as representative of control. Dot- ted black line indicates threshold for “hit” selection set to Z score $ 3. (B) Western blot showing increased fully glycosylated protein (mature), representative of increased KV11.1 protein trafficking after 24-hour treatment with 10 mM azelastine, azaperone, or ibutilide. All wells loaded with 20 mg of protein. (C) Western blot showing increased KV11.1 protein trafficking after 24 hours of treatment with 10 mM azelastine, azaper- one, or ibutilide in HEK-293 cells expressing KV11.1-N470D and KV11.1-G601S. All wells loaded with 20 mg of protein. (D) Whole cell current recordings at 120 mV step. Representative current traces (left) and bar graphs (right) depicting KV11.1-G601S-G965*X current after 24-hour incubation with 10 mM drug and washout before experiments. Inset shows enlarged current traces at 120 mV voltage step. N 5 8 for E-4031 treatment and n 5 7 for all other treatments. Treated samples compared with vehicle control (0.1% DMSO) by one-way ANOVA with post hoc Dunnett’s t test. Bars on scatter plots represent mean of each group. * 5 P < 0.05. Veh. 5 0.1% DMSO, E-4. 5 E-4031, Azel. 5 azelastine, Azap. 5 azaperone, and Ibu. 5 ibutilide.

Article Snippet: Ibutilide, gabapentin, and azaperone were purchased from SelleckChem, Azelastine and VU0405601 were purchased from Millipore Sigma, and Cesium gluconate was purchased from HelloBio, all as dry powder.

Techniques: Flux Assay, Control, Selection, Western Blot, Expressing, Incubation

Journal: Cell Reports Medicine

Article Title: Use of Patient Health Records to Quantify Drug-Related Pro-arrhythmic Risk

doi: 10.1016/j.xcrm.2020.100076

Figure Lengend Snippet: Ranking of CiPA Drugs by Disproportionality (EB05) for Cardiac Adverse Events

Article Snippet: IBUTILIDE , TargetMol , T6541; CAS 122647-32-9.

Techniques: Blocking Assay

Journal: Cell Reports Medicine

Article Title: Use of Patient Health Records to Quantify Drug-Related Pro-arrhythmic Risk

doi: 10.1016/j.xcrm.2020.100076

Figure Lengend Snippet:

Article Snippet: IBUTILIDE , TargetMol , T6541; CAS 122647-32-9.

Techniques: Recombinant, Software