stresnil Search Results


azaperone  (Selleck Chemicals)
90
Selleck Chemicals azaperone
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, <t>azaperone,</t> 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.
Azaperone, supplied by Selleck Chemicals, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pm35125346-163-3-7?v=Selleck+Chemicals
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11885084 hbss gibco  (Thermo Fisher)
91
Thermo Fisher 11885084 hbss gibco
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, <t>azaperone,</t> 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.
11885084 Hbss Gibco, supplied by Thermo Fisher, used in various techniques. Bioz Stars score: 91/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pm36493752-247-64-66?v=Thermo+Fisher
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avetlabs n a azaperone chiron 13849 19 optixcare eye lube aventix animal health opx 4242 lidocaine hci injection with preservative  (ZeptoMetrix corporation)
93
ZeptoMetrix corporation avetlabs n a azaperone chiron 13849 19 optixcare eye lube aventix animal health opx 4242 lidocaine hci injection with preservative
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, <t>azaperone,</t> 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.
Avetlabs N A Azaperone Chiron 13849 19 Optixcare Eye Lube Aventix Animal Health Opx 4242 Lidocaine Hci Injection With Preservative, supplied by ZeptoMetrix corporation, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pm36493752-247-96-99?v=ZeptoMetrix+corporation
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stresnil neuroleptic injection for pigs  (Ausrichter Pty Ltd)
90
Ausrichter Pty Ltd stresnil neuroleptic injection for pigs
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, <t>azaperone,</t> 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.
Stresnil Neuroleptic Injection For Pigs, supplied by Ausrichter Pty Ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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azaperone stresnil  (Ecuphar GmbH)
90
Ecuphar GmbH azaperone stresnil
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, <t>azaperone,</t> 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.
Azaperone Stresnil, supplied by Ecuphar GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pmc09525691-188-5-14?v=Ecuphar+GmbH
Average 90 stars, based on 1 article reviews
azaperone stresnil - by Bioz Stars, 2026-08
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azaperone  (Richter Pharma AG)
90
Richter Pharma AG azaperone
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, <t>azaperone,</t> 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.
Azaperone, supplied by Richter Pharma AG, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pmc10230747-67-15-20?v=Richter+Pharma+AG
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azaperone - by Bioz Stars, 2026-08
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stresnil  (China Chemical and Pharmaceutical)
90
China Chemical and Pharmaceutical stresnil
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, <t>azaperone,</t> 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.
Stresnil, supplied by China Chemical and Pharmaceutical, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/stresnil/pmc06695206-211-5-6?v=China+Chemical+and+Pharmaceutical
Average 90 stars, based on 1 article reviews
stresnil - by Bioz Stars, 2026-08
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stresnil  (Bayer Animal Health GmbH)
90
Bayer Animal Health GmbH stresnil
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, <t>azaperone,</t> 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.
Stresnil, supplied by Bayer Animal Health GmbH, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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sedation stresnil 2.5 ml/kg  (Vetoquinol sa)
90
Vetoquinol sa sedation stresnil 2.5 ml/kg
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, <t>azaperone,</t> 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.
Sedation Stresnil 2.5 Ml/Kg, supplied by Vetoquinol sa, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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azaperone stresnil  (Vetoquinol sa)
90
Vetoquinol sa azaperone stresnil
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, <t>azaperone,</t> 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.
Azaperone Stresnil, supplied by Vetoquinol sa, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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azaperone (stresnil  (Schering-Plough corporation)
90
Schering-Plough corporation azaperone (stresnil
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, <t>azaperone,</t> 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.
Azaperone (Stresnil, supplied by Schering-Plough corporation, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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azaperone stresnil ad usum veterinarium  (Sanochemia ag)
90
Sanochemia ag azaperone stresnil ad usum veterinarium
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, <t>azaperone,</t> 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.
Azaperone Stresnil Ad Usum Veterinarium, supplied by Sanochemia ag, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Image Search Results


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.

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