CFTR
信号経路図
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S6003 | Ataluren (PTC124) | <1 mg/mL | 57 mg/mL | <1 mg/mL |
| S1144 | Ivacaftor (VX-770) | <1 mg/mL | 78 mg/mL | <1 mg/mL |
| S1565 | VX-809 (Lumacaftor) | <1 mg/mL | 90 mg/mL | 6 mg/mL |
| S7059 | Tezacaftor (VX-661) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1675 | Lubiprostone | <1 mg/mL | 78 mg/mL | 78 mg/mL |
| S7139 | CFTRinh-172 | <1 mg/mL | 82 mg/mL | <1 mg/mL |
| S7329 | IOWH032 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8094 | GlyH-101 | <1 mg/mL | 98 mg/mL | <1 mg/mL |
- CFTR阻害剤(4)
- CFTR活性剤(2)
- CFTRモジュレータ(2)
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S6003 |
Ataluren (PTC124)Ataluren (PTC124)は、~0.1μMのEC50による強力なナンセンス変異阻害剤です。 |
Effect of systemic ataluren treatment on mice with the Pax6Sey+/- phenotype. The black arrowhead indicates the lenticular stalk; the black arrow indicates the cornea; and the asterisk indicates the ciliary margin. WT, Pax6+/+; Mt, Pax6Sey/+; L, lens; r, retina. Original magnification, x5.
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| S7139 |
CFTRinh-172CFTRinh-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. |
CFTR attenuated ox-LDL-induced NF-
|
|
| S7329 |
IOWH032IOWH032 is a synthetic CFTR inhibitor. Phase 1/2. |
||
| S8094 |
GlyH-101 |
||
| S1565 |
VX-809 (Lumacaftor)VX-809 (Lumacaftor)は、0.1μMのEC50による嚢胞性線維症膜内外コンダクタンス監査機関（CFTR）モジュレータです。 |
△F508CFTR diffusion is increased by different correction mechanisms. A, example trajectories from MDCK cell lines for wtCFTR (black) and △F508CFTR rescued by VX-809 treatment in the absence (red) and presence (blue ) of mCh-CFTR-C. B, summary graph for wtCFTR, r△F508CFTR and CFTR△PDZ diffusion in VX-809-treated and control MDCK cell lines. C, example trajectories for MDCK cells transiently expressing 3FLAG-tagged wtCFTR(black), △F508CFTR rescued by VX-809 (red), CFTR△PDZ ( blue ), and △F508CFTR△PDZ rescued by VX-809 (green). D, summary graph for CFTR dif- fusion in VX-809-treated MDCK transiently transfected with 3FLAG-tagged CFTR constructs. E, example trajectories from MDCK cell lines stably expressing wtCFTR ( left ) and △F508CFTR ( right ) treated with thapsigargin ( black)or CoPo-22 (red) or transiently expressing GFP-GRASP55 (blue ). F, graphs for △F508CFTR ( top ) and wtCFTR (bottom) diffusion in MDCK cell lines treated with thapsigargin or CoPo-22 or transiently expressing GFP-GRASP55. For reference, median and interquartile values for wtCFTR diffusive range are shown by dashed lines(bar 1, top ). G, GFP-GRASP55 is Golgi-localized by immunocytochemical analysis (scale bar, 10 μm). Scale bar in A (500 nm) refers to all trajectories. In panels Band D, statistically significant differences in populations are shown (*, p<0.001). SPT data for MDCK cell lines was derived from 140 –788 trajectories and for transiently transfected MDCK cells from 131–298 trajectories. |
|
| S7059 |
Tezacaftor (VX-661)Tezacaftor (VX-661)は、第F508del CFTR に補正され、CFTRタンパク質は細胞表面に達するのを助けると考えられている。 |
(B)ΔISC response to forskolin observed in VX-661-treated CF HBE cells (*P = 0.0021, VX661 vs. vehicle) was prevented by chronic VX-770 treatment and significantly different from VX-661-treated cells (#P=0.0126, VX661 vs. VX661+VX770). (C) The response to CFTR inh-172 that was observed in VX-661-treated cells (*P = 0.0111, VX661 vs. vehicle) was significantly decreased in VX809+VX770 treated cells (#P = 0.0038, VX661 vs. VX661+VX770). Primary CF HBE cultures (ΔF508/ΔF508) were derived from 3 different patients, and 3-4 replicates were performed per patient.
|
|
| S1144 |
Ivacaftor (VX-770)Ivacaftor (VX-770)は、G551D-CFTRとF508del-CFTRを目標としている嚢胞性線維症膜内外コンダクタンス監査機関（CFTR）の強化剤で、EC50 がそれぞれ 100 nM と 25 nMです。 |
(A) CFTR Western blot of normal (NL) and CF HBE cultures treated with VX-809 (5 uM) ± VX-770 (5 uM) for 48 hours. “*” indicates the mature, complex glycosylated form of CFTR, band C; “•” indicates the immature band B. (B) Turnover of rescued ΔF508 in BHK-21 cells. ΔF508 was rescued at 27°C in the presence of VX-809 ± VX-770 for 24 hours. After adding cycloheximide (200 ug/ml, 37°C), cells were lysed at the indicated times and analyzed by Western blotting.
|
|
| S1675 |
LubiprostoneLubiprostone(Amitiza) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation. |
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S6003 |
Ataluren (PTC124)Ataluren (PTC124)は、~0.1μMのEC50による強力なナンセンス変異阻害剤です。 |
Effect of systemic ataluren treatment on mice with the Pax6Sey+/- phenotype. The black arrowhead indicates the lenticular stalk; the black arrow indicates the cornea; and the asterisk indicates the ciliary margin. WT, Pax6+/+; Mt, Pax6Sey/+; L, lens; r, retina. Original magnification, x5.
|
|
| S7139 |
CFTRinh-172CFTRinh-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. |
CFTR attenuated ox-LDL-induced NF-
|
|
| S7329 |
IOWH032IOWH032 is a synthetic CFTR inhibitor. Phase 1/2. |
||
| S8094 |
GlyH-101 |
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S1144 |
Ivacaftor (VX-770)Ivacaftor (VX-770)は、G551D-CFTRとF508del-CFTRを目標としている嚢胞性線維症膜内外コンダクタンス監査機関（CFTR）の強化剤で、EC50 がそれぞれ 100 nM と 25 nMです。 |
2014, 6(246):246ra96 2015, 10(3):363-81 2012, 186(7):694-6 |
(A) CFTR Western blot of normal (NL) and CF HBE cultures treated with VX-809 (5 uM) ± VX-770 (5 uM) for 48 hours. “*” indicates the mature, complex glycosylated form of CFTR, band C; “•” indicates the immature band B. (B) Turnover of rescued ΔF508 in BHK-21 cells. ΔF508 was rescued at 27°C in the presence of VX-809 ± VX-770 for 24 hours. After adding cycloheximide (200 ug/ml, 37°C), cells were lysed at the indicated times and analyzed by Western blotting.
|
| S1675 |
LubiprostoneLubiprostone(Amitiza) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation. |
| 製品コード | 製品説明 | 文献中の使用例 | お客様のフィードバック |
|---|---|---|---|
| S1565 |
VX-809 (Lumacaftor)VX-809 (Lumacaftor)は、0.1μMのEC50による嚢胞性線維症膜内外コンダクタンス監査機関（CFTR）モジュレータです。 |
2013, 19(7):939-45 2014, 6(246):246ra96 2015, 10(3):363-81 |
△F508CFTR diffusion is increased by different correction mechanisms. A, example trajectories from MDCK cell lines for wtCFTR (black) and △F508CFTR rescued by VX-809 treatment in the absence (red) and presence (blue ) of mCh-CFTR-C. B, summary graph for wtCFTR, r△F508CFTR and CFTR△PDZ diffusion in VX-809-treated and control MDCK cell lines. C, example trajectories for MDCK cells transiently expressing 3FLAG-tagged wtCFTR(black), △F508CFTR rescued by VX-809 (red), CFTR△PDZ ( blue ), and △F508CFTR△PDZ rescued by VX-809 (green). D, summary graph for CFTR dif- fusion in VX-809-treated MDCK transiently transfected with 3FLAG-tagged CFTR constructs. E, example trajectories from MDCK cell lines stably expressing wtCFTR ( left ) and △F508CFTR ( right ) treated with thapsigargin ( black)or CoPo-22 (red) or transiently expressing GFP-GRASP55 (blue ). F, graphs for △F508CFTR ( top ) and wtCFTR (bottom) diffusion in MDCK cell lines treated with thapsigargin or CoPo-22 or transiently expressing GFP-GRASP55. For reference, median and interquartile values for wtCFTR diffusive range are shown by dashed lines(bar 1, top ). G, GFP-GRASP55 is Golgi-localized by immunocytochemical analysis (scale bar, 10 μm). Scale bar in A (500 nm) refers to all trajectories. In panels Band D, statistically significant differences in populations are shown (*, p<0.001). SPT data for MDCK cell lines was derived from 140 –788 trajectories and for transiently transfected MDCK cells from 131–298 trajectories. |
| S7059 |
Tezacaftor (VX-661)Tezacaftor (VX-661)は、第F508del CFTR に補正され、CFTRタンパク質は細胞表面に達するのを助けると考えられている。 |
2014, 6(246):246ra96 2017, 10.1038/s41525-017-0015-6 |
(B)ΔISC response to forskolin observed in VX-661-treated CF HBE cells (*P = 0.0021, VX661 vs. vehicle) was prevented by chronic VX-770 treatment and significantly different from VX-661-treated cells (#P=0.0126, VX661 vs. VX661+VX770). (C) The response to CFTR inh-172 that was observed in VX-661-treated cells (*P = 0.0111, VX661 vs. vehicle) was significantly decreased in VX809+VX770 treated cells (#P = 0.0038, VX661 vs. VX661+VX770). Primary CF HBE cultures (ΔF508/ΔF508) were derived from 3 different patients, and 3-4 replicates were performed per patient.
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