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cftr inh172  (Merck & Co)

 
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    Structured Review

    Merck & Co cftr inh172
    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR <t>inh172</t> for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.
    Cftr Inh172, supplied by Merck & Co, 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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    Images

    1) Product Images from "Expression of Wild-Type CFTR Suppresses NF-κB-Driven Inflammatory Signalling"

    Article Title: Expression of Wild-Type CFTR Suppresses NF-κB-Driven Inflammatory Signalling

    Journal: PLoS ONE

    doi: 10.1371/journal.pone.0011598

    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR inh172 for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.
    Figure Legend Snippet: A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR inh172 for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.

    Techniques Used: Activity Assay, Transfection, Plasmid Preparation, Enzyme-linked Immunosorbent Assay

    Related Articles

    Transfection:

    Article Title: Expression of Wild-Type CFTR Suppresses NF-κB-Driven Inflammatory Signalling
    Article Snippet: .. 24 h post transfection, cells were treated with combinations of 10 ng/ml TNFα, to stimulate NF-κB activity, 10 μM CFTR inh172 (Merck, Nottingham, U.K.), to inhibit CFTR and 10 μM Forskolin and 10 μM IBMX to stimulate PKA by elevating cAMP. ..

    Activity Assay:

    Article Title: Expression of Wild-Type CFTR Suppresses NF-κB-Driven Inflammatory Signalling
    Article Snippet: .. 24 h post transfection, cells were treated with combinations of 10 ng/ml TNFα, to stimulate NF-κB activity, 10 μM CFTR inh172 (Merck, Nottingham, U.K.), to inhibit CFTR and 10 μM Forskolin and 10 μM IBMX to stimulate PKA by elevating cAMP. ..



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    Following overnight incubation in S-VX-121 ( A; 1 μM) or R-VX-121 ( B; 1 μM), forskolin (10 μM) and VX-770 (1 μM) induced an increase in I Cl that was inhibited by CFTR <t>inh172</t> (3 μM). C. Average responses to forskolin + VX-770 for experiments in A and B. DMSO (0.1%) was used as a control. D. Immunoblot of CFTR showing correction of F508del CFTR by S-VX-121, but not R-VX-121. E. Average results for 3 experiments. F. Cl − currents in response to forskolin following overnight incubation in S-VX-121 (1 μM; blue trace) or S-VX-121 (1 μM) plus R-VX-121 (3 μM) (red trace). G. Concentration-response relationship for inhibition of S-VX-121-induced correction of I Cl by R-VX-121. The data were fit to the Hill equation with an apparent IC 50 of 3.5 μM. H. Cl − currents in response to forskolin following overnight incubation in VX-445 (1 μM; blue trace) or VX-445 (1 μM) plus R-VX-121 (6 μM) (red trace). I. Average response to forskolin for the experiments shown in H (n=23). J, K, L. F508del CFTR was corrected with VX-445 (1 μM) plus VX-661 (3 μM). Forskolin was used to stimulate I Cl and the effect of VX-770 (1 μM; J ), S-VX-121 (10 μM) followed by VX-770 ( K ) or R-VX-121 (10 μM) followed by VX-770 ( L ) determined. CFTR inh172 (3 μM) was used to confirm I Cl was due to CFTR. M. Chemical structures of VX-770, S-VX-121 and R-VX-121. #, P<0.01.
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    Rescue of functional p.Phe508del-CFTR Cl− currents in Kaftrio ® - or Orkambi ® -treated CFBE 41o- cells. Representative whole-cell Cl − current traces were elicited by voltage steps from a holding potential of −40 mV to a series of test potentials ranging from 0 to +60 mV in 20 mV increments every 10 s in CFBE 41o- cells expressing wt-CFTR (column A ) or p.Phe508del-CFTR (column B ) or in cells expressing deletion mutant CFTR but treated for 24 h with LUM/IVA (column C ) or ELX/TEZ/IVA (column D ) for 24 h. The duration of the depolarizing pulses was 1 s. For clarity, Cl − currents recorded at 0 mV are shown throughout the figure. Top panels : basal currents recorded at 0 mV in the absence of FSK/IBMX stimulation (black), recorded upon ∼2 min stimulation by FSK/IBMX (10/100 μM) (blue) and in the presence of FSK/IBMX and 20 μM of CFTR <t>inh172</t> (red). The middle panels show the corresponding peak current densities determined at 0 mV (pA/pF, mean ± SEM) obtained in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). The current density for a particular cell was determined as the average of current density values obtained for three to four consecutive depolarizing pulses repeated every 5 s. Bottom panels: current density–voltage relationships (pA/pF, mean ± SEM) measured at the indicated test potentials in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). ( E ) Analysis of the basal peak current densities (pA/pF) determined at +40 mV and recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( F ) Analysis of the FSK (10 µM)/IBMX (100 µM)-stimulated peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment ( p.Phe508del-CFTR , empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( G ) Analysis of the FSK/IBMX-stimulated and CFTR inh172 (20 µM)-inhibited peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). Data are expressed as mean ± SEM (n = 7–16 cells/condition) unless otherwise indicated, and each symbol represents an individual record. An unpaired or paired t-test was performed for comparisons. Differences were considered significant at p < 0.05 (*), p < 0.01 (**), p < 0.001 (***), and p < 0.0001 (****).
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    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR <t>inh172</t> for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.
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    cftr inhibitor, cftr-inh172  (Millipore)
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    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR <t>inh172</t> for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.
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    cftr-inh172  (Millipore)
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    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR <t>inh172</t> for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.
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    Image Search Results


    Following overnight incubation in S-VX-121 ( A; 1 μM) or R-VX-121 ( B; 1 μM), forskolin (10 μM) and VX-770 (1 μM) induced an increase in I Cl that was inhibited by CFTR inh172 (3 μM). C. Average responses to forskolin + VX-770 for experiments in A and B. DMSO (0.1%) was used as a control. D. Immunoblot of CFTR showing correction of F508del CFTR by S-VX-121, but not R-VX-121. E. Average results for 3 experiments. F. Cl − currents in response to forskolin following overnight incubation in S-VX-121 (1 μM; blue trace) or S-VX-121 (1 μM) plus R-VX-121 (3 μM) (red trace). G. Concentration-response relationship for inhibition of S-VX-121-induced correction of I Cl by R-VX-121. The data were fit to the Hill equation with an apparent IC 50 of 3.5 μM. H. Cl − currents in response to forskolin following overnight incubation in VX-445 (1 μM; blue trace) or VX-445 (1 μM) plus R-VX-121 (6 μM) (red trace). I. Average response to forskolin for the experiments shown in H (n=23). J, K, L. F508del CFTR was corrected with VX-445 (1 μM) plus VX-661 (3 μM). Forskolin was used to stimulate I Cl and the effect of VX-770 (1 μM; J ), S-VX-121 (10 μM) followed by VX-770 ( K ) or R-VX-121 (10 μM) followed by VX-770 ( L ) determined. CFTR inh172 (3 μM) was used to confirm I Cl was due to CFTR. M. Chemical structures of VX-770, S-VX-121 and R-VX-121. #, P<0.01.

    Journal: American journal of physiology. Cell physiology

    Article Title: (R)-vanzacaftor potentiates BK Ca channels in the absence of CFTR correction or potentiation

    doi: 10.1152/ajpcell.00654.2025

    Figure Lengend Snippet: Following overnight incubation in S-VX-121 ( A; 1 μM) or R-VX-121 ( B; 1 μM), forskolin (10 μM) and VX-770 (1 μM) induced an increase in I Cl that was inhibited by CFTR inh172 (3 μM). C. Average responses to forskolin + VX-770 for experiments in A and B. DMSO (0.1%) was used as a control. D. Immunoblot of CFTR showing correction of F508del CFTR by S-VX-121, but not R-VX-121. E. Average results for 3 experiments. F. Cl − currents in response to forskolin following overnight incubation in S-VX-121 (1 μM; blue trace) or S-VX-121 (1 μM) plus R-VX-121 (3 μM) (red trace). G. Concentration-response relationship for inhibition of S-VX-121-induced correction of I Cl by R-VX-121. The data were fit to the Hill equation with an apparent IC 50 of 3.5 μM. H. Cl − currents in response to forskolin following overnight incubation in VX-445 (1 μM; blue trace) or VX-445 (1 μM) plus R-VX-121 (6 μM) (red trace). I. Average response to forskolin for the experiments shown in H (n=23). J, K, L. F508del CFTR was corrected with VX-445 (1 μM) plus VX-661 (3 μM). Forskolin was used to stimulate I Cl and the effect of VX-770 (1 μM; J ), S-VX-121 (10 μM) followed by VX-770 ( K ) or R-VX-121 (10 μM) followed by VX-770 ( L ) determined. CFTR inh172 (3 μM) was used to confirm I Cl was due to CFTR. M. Chemical structures of VX-770, S-VX-121 and R-VX-121. #, P<0.01.

    Article Snippet: Paxilline (HY-N6778), VX-445 (HY-111772), S-VX-121 (HY-145603), R-VX-121 (HY-145603A) and CFTR inh172 (HY-16671) were obtained from MedChemExpress.

    Techniques: Incubation, Control, Western Blot, Concentration Assay, Inhibition

    A. Concentration-dependent vasodilation of mesenteric artery by R-VX-121 from a male mouse. B. Average responses in male mice to S- (blue line, n=7) and R- (red line, n=7) VX-121. C and D . Average responses in male mice to R-VX-121 ( C ) and S-VX-121 ( D ) under control conditions (solid lines) and in the presence of 10 μM paxilline (Pax; dashed lines). Paxilline inhibited the response to both R- and S-VX-121 (n=8 for all conditions, P<0.01). E. Average responses in female mice to S- (blue line, n=7) and R- (red line, n=7) VX-121. F and G. Average responses in male mice to S-VX-121 ( F ) and R-VX-121 ( G ) under control conditions (solid lines) and in the presence of 3 μM CFTR inh172 (dashed lines). CFTR inh172 had no effect (n=8 for all conditions).

    Journal: American journal of physiology. Cell physiology

    Article Title: (R)-vanzacaftor potentiates BK Ca channels in the absence of CFTR correction or potentiation

    doi: 10.1152/ajpcell.00654.2025

    Figure Lengend Snippet: A. Concentration-dependent vasodilation of mesenteric artery by R-VX-121 from a male mouse. B. Average responses in male mice to S- (blue line, n=7) and R- (red line, n=7) VX-121. C and D . Average responses in male mice to R-VX-121 ( C ) and S-VX-121 ( D ) under control conditions (solid lines) and in the presence of 10 μM paxilline (Pax; dashed lines). Paxilline inhibited the response to both R- and S-VX-121 (n=8 for all conditions, P<0.01). E. Average responses in female mice to S- (blue line, n=7) and R- (red line, n=7) VX-121. F and G. Average responses in male mice to S-VX-121 ( F ) and R-VX-121 ( G ) under control conditions (solid lines) and in the presence of 3 μM CFTR inh172 (dashed lines). CFTR inh172 had no effect (n=8 for all conditions).

    Article Snippet: Paxilline (HY-N6778), VX-445 (HY-111772), S-VX-121 (HY-145603), R-VX-121 (HY-145603A) and CFTR inh172 (HY-16671) were obtained from MedChemExpress.

    Techniques: Concentration Assay, Control

    Rescue of functional p.Phe508del-CFTR Cl− currents in Kaftrio ® - or Orkambi ® -treated CFBE 41o- cells. Representative whole-cell Cl − current traces were elicited by voltage steps from a holding potential of −40 mV to a series of test potentials ranging from 0 to +60 mV in 20 mV increments every 10 s in CFBE 41o- cells expressing wt-CFTR (column A ) or p.Phe508del-CFTR (column B ) or in cells expressing deletion mutant CFTR but treated for 24 h with LUM/IVA (column C ) or ELX/TEZ/IVA (column D ) for 24 h. The duration of the depolarizing pulses was 1 s. For clarity, Cl − currents recorded at 0 mV are shown throughout the figure. Top panels : basal currents recorded at 0 mV in the absence of FSK/IBMX stimulation (black), recorded upon ∼2 min stimulation by FSK/IBMX (10/100 μM) (blue) and in the presence of FSK/IBMX and 20 μM of CFTR inh172 (red). The middle panels show the corresponding peak current densities determined at 0 mV (pA/pF, mean ± SEM) obtained in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). The current density for a particular cell was determined as the average of current density values obtained for three to four consecutive depolarizing pulses repeated every 5 s. Bottom panels: current density–voltage relationships (pA/pF, mean ± SEM) measured at the indicated test potentials in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). ( E ) Analysis of the basal peak current densities (pA/pF) determined at +40 mV and recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( F ) Analysis of the FSK (10 µM)/IBMX (100 µM)-stimulated peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment ( p.Phe508del-CFTR , empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( G ) Analysis of the FSK/IBMX-stimulated and CFTR inh172 (20 µM)-inhibited peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). Data are expressed as mean ± SEM (n = 7–16 cells/condition) unless otherwise indicated, and each symbol represents an individual record. An unpaired or paired t-test was performed for comparisons. Differences were considered significant at p < 0.05 (*), p < 0.01 (**), p < 0.001 (***), and p < 0.0001 (****).

    Journal: Journal of Clinical Medicine

    Article Title: Comparison of the Effect of CFTR Modulators elexacaftor / tezacaftor / ivacaftor and lumacaftor / ivacaftor via Serum Human Epididymis Protein 4 Concentration in p.Phe508del-CFTR Homozygous Cystic Fibrosis Patients

    doi: 10.3390/jcm14176188

    Figure Lengend Snippet: Rescue of functional p.Phe508del-CFTR Cl− currents in Kaftrio ® - or Orkambi ® -treated CFBE 41o- cells. Representative whole-cell Cl − current traces were elicited by voltage steps from a holding potential of −40 mV to a series of test potentials ranging from 0 to +60 mV in 20 mV increments every 10 s in CFBE 41o- cells expressing wt-CFTR (column A ) or p.Phe508del-CFTR (column B ) or in cells expressing deletion mutant CFTR but treated for 24 h with LUM/IVA (column C ) or ELX/TEZ/IVA (column D ) for 24 h. The duration of the depolarizing pulses was 1 s. For clarity, Cl − currents recorded at 0 mV are shown throughout the figure. Top panels : basal currents recorded at 0 mV in the absence of FSK/IBMX stimulation (black), recorded upon ∼2 min stimulation by FSK/IBMX (10/100 μM) (blue) and in the presence of FSK/IBMX and 20 μM of CFTR inh172 (red). The middle panels show the corresponding peak current densities determined at 0 mV (pA/pF, mean ± SEM) obtained in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). The current density for a particular cell was determined as the average of current density values obtained for three to four consecutive depolarizing pulses repeated every 5 s. Bottom panels: current density–voltage relationships (pA/pF, mean ± SEM) measured at the indicated test potentials in the absence of FSK/IBMX (basal, black symbols), upon stimulation by FSK/IBMX (blue symbols), and in the presence of FSK/IBMX and 20 μM CFTR inh172 (red symbols). ( E ) Analysis of the basal peak current densities (pA/pF) determined at +40 mV and recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( F ) Analysis of the FSK (10 µM)/IBMX (100 µM)-stimulated peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment ( p.Phe508del-CFTR , empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). ( G ) Analysis of the FSK/IBMX-stimulated and CFTR inh172 (20 µM)-inhibited peak current densities (pA/pF) recorded in cells in the absence of CFTRm pretreatment (F580del, empty circles), pre-treated with LUM/IVA (up triangles) or ELX/TEZ/IVA (down triangles). Data are expressed as mean ± SEM (n = 7–16 cells/condition) unless otherwise indicated, and each symbol represents an individual record. An unpaired or paired t-test was performed for comparisons. Differences were considered significant at p < 0.05 (*), p < 0.01 (**), p < 0.001 (***), and p < 0.0001 (****).

    Article Snippet: CFTR correctors elexacaftor (VX-445) (S8851), lumacaftor (VX-809) (S1565), and tezacaftor (VX-661) (S7059); CFTR potentiator ivacaftor (VX-770) (S1144); voltage-independent selective CFTR inhibitor CFTR inh172 (S7139); and CFTR activator (FSK, S2449) were purchased from Selleck Chemicals (Houston, TX, USA). cAMP phosphodiesterase inhibitor IBMX (I5879) was ordered from Sigma-Aldrich (St. Louis, MO, USA).

    Techniques: Functional Assay, Expressing, Mutagenesis

    A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR inh172 for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.

    Journal: PLoS ONE

    Article Title: Expression of Wild-Type CFTR Suppresses NF-κB-Driven Inflammatory Signalling

    doi: 10.1371/journal.pone.0011598

    Figure Lengend Snippet: A . NF-κB activity in H441 cells transfected with either empty vector or wt-CFTR (400 ng), each treated with 10 µM CFTR inh172 for 4 hours, n = 3 *p<0.05 (compared to empty vector control), # p<0.05 (compared to CFTR control). B . NF-κB activity in 16HBE14o − cells treated with 10 µM CFTR inh172 and/or 10 µM forskolin and 100 µM IBMX for 4 h, n = 7, *p<0.05. C . IL-8 levels in supernatants from 16HBE14o − cells measured by ELISA, n = 8, p not significant. D IL-8 levels in supernatants from primary human nasal epithelial cells treated with 10 µM CFTR inh172 for 4 hours, n = 4, *p<0.05.

    Article Snippet: 24 h post transfection, cells were treated with combinations of 10 ng/ml TNFα, to stimulate NF-κB activity, 10 µM CFTR inh172 (Merck, Nottingham, U.K.), to inhibit CFTR and 10 µM Forskolin and 10 µM IBMX to stimulate PKA by elevating cAMP.

    Techniques: Activity Assay, Transfection, Plasmid Preparation, Enzyme-linked Immunosorbent Assay