The ATP-binding cassette (ABC) transporter family includes the CFTR (Cystic Fibrosis Transmembrane Conductance Regulator), which functions as a channel for small anions like chloride and bicarbonate. Two identical halves of CFTR, each with a transmembrane (TMD) and a nucleotide binding domain (NBD), make up the entire structure. The cytosolic regulatory (R) domain of CFTR is phosphorylated, and ATP is bound and hydrolyzed at two NBDs to control CFTR activity.
Although CFTR is expressed in a wide variety of cell types throughout the body, it is primarily found in the secretory serous cells of the submucosal glands in the airways. The cytosolic nucleotide binding domains of CFTR are coupled with the transmembrane (TM) domains to form the pathway for anion permeation, and ATP binding and hydrolysis on these domains controls transitions between open and closed states. CFTR activity is typically tightly regulated because dysregulation can result in fatal conditions like cystic fibrosis and secretory diarrhoea.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74172 | (R)-Elexacaftor ((R)-VX-445) | 2229860-99-3 | (R)-Elexacaftor is the enantiomer of Elexacaftor (Compound 1), derived from Compound 37 in patent WO2018107100A1. |
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V74180 | (R)-Olacaftor ((R)-VX-440) | 1899111-41-1 | (R)-Olacaftor ((R)-VX-440) is a cystic fibrosis transmembrane regulator (CFTR) modulator. |
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V74181 | (R)-Posenacaftor sodium ((R)-PTI-801 sodium) | 2095064-09-6 | (R)-Posenacaftor (R)-PTI-801) sodium is the R enantiomer of Posenacaftor. |
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V74179 | (Rac)-Tezacaftor ((Rac)-VX-661) | 1226709-85-8 | (Rac)-Tezacaftor ((Rac)-VX-661) is the racemate of Tezacaftor. |
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V74163 | Astressin 2B | 681260-70-8 | Astressin 2B is a potent and specific corticotropin-releasing factor receptor 2 (CRF2) antagonist (inhibitor) with IC50s of 1.3 and >500 nM for CRF2 and CRF1, respectively. |
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V74177 | CFTR corrector 11 | 688050-45-5 | CFTR corrector 11 (compound 133) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. |
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V74164 | CFTR corrector 12 | 958941-60-1 | CFTR corrector 12 (compound 17C) is a bisthiazole analogue used as a CFTR corrector. |
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V74169 | CFTR corrector 6 | 2226970-01-8 | CFTR corrector 6 is a potent cystic fibrosis transmembrane conductance regulator (CFTR) enhancer. |
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V74176 | CFTR corrector 8 | 1918142-35-4 | CFTR corrector 8 is an efficient CFTR modulator. |
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V74178 | CFTRactivator 1 | 2768261-09-0 | CFTR activator 1 is a potent and specific CFTR activator with EC50 of 23 nM. |
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V74174 | CP-628006 | 305822-08-6 | CP-628006 is a CFTR small molecule enhancer that restores the ATP-dependent gating channel of the cystic fibrosis mutant G551D-CFTR. |
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V74165 | CRF1 receptor antagonist-1 | 2635364-30-4 | CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. |
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V10043 | Elexacaftor (VX-445, WHO-11180) | 2216712-66-0 | Elexacaftor (VX-445, WHO-11180; WHO11180; VX445;Kaftrio;Trikafta)is one of three components in thefixed-dose combination medication (Elexacaftor/tezacaftor/ivacaftor, trade name: Trikafta and Kaftrio) used in patients who have cystic fibrosis with a F508del mutation. |
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V3551 | FDL-169 | 1628416-28-3 | FDL-169 is a novel and potent CFTR (Cystic fibrosis transmembrane conductance regulator) correctorbeing developed by Flatley Discovery Lab for treating cystic fibrosis (CF) patients who carry the F508del mutation, the most common mutation in this disease. |
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V4568 | GLPG-1837 | 1654725-02-6 | GLPG1837 (also known as ABBV-974) is a novel, potent and reversibleCFTR(cystic fibrosis transmembrane conductance regulator) potentiator withEC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. |
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V20997 | GlyH-101 | 328541-79-3 | GlyH-101 is a novel and potent CFTR inhibitor (cystic fibrosis transmembrane conductance regulator) with Ki of 1.4 uM. |
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V3900 | Ivacaftor benzenesulfonate (VX770) | 1134822-09-5 | Ivacaftor (also known as VX-770; trade name:KALYDECO andSymdeko) is a potent and orally active potentiator of CFTR (cystic fibrosis transmembrane conductance regulator) targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively. |
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V3901 | Ivacaftor hydrate (VX-770) | 1134822-07-3 | Ivacaftor (also known as VX-770; trade name:KALYDECO andSymdeko) is a potent and orally bioactive potentiator of CFTR (cystic fibrosis transmembrane conductance regulator) targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively. |
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V76876 | Ivacaftor-d4 (Ivacaftor-d4; VX-770-d4) | Ivacaftor-d4 (VX-770-d4) is a deuterium labelled form of Ivacaftor. | |
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V76856 | K41498 TFA | K41498 TFA is a selective CRF2 receptor antagonist (inhibitor) with Kis of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. |
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