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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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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V3004 | KM 11060 | 774549-97-2 | KM11060 is a novel mutated corrector of the F508del-CFTR (cystic fibrosis transmembrane conductance regulator) trafficking defect. |
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V74170 | Kobusin (spin escin) | 36150-23-9 | Kobusin is a diepoxy lignan extracted from Pnonobio biondii Pamp. |
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V51294 | Navocaftor (GLPG-3067; ABBV-3067) | 2159103-66-7 | Navocaftor (GLPG 3067), a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, Example 1). |
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V74167 | NJH-2-057 | 2858812-70-9 | NJH-2-057 is a conjugate of the deubiquitinase OTUB1 covalently linked to lumacaftor, which stabilizes mutated CFTR protein in cells. |
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V74175 | Posenacaftor (PTI-801) | 2095064-05-2 | Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulatory protein (CFTR) modulator that corrects the folding and trafficking of CFTR protein. |
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V74166 | Posenacaftor sodium (PTI-801 sodium) | 2095064-06-3 | Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulatory protein (CFTR) modulator that corrects the folding and trafficking of CFTR protein. |
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V2875 | PPQ-102 | 931706-15-9 | PPQ-102 (also known as CFTR Inhibitor) is a potentinhibitor of CFTR (cystic fibrosis transmembrane conductance regulator) discovered from screening of approximately 110000 small synthetic and natural compounds for inhibition of halide influx in CFTR-expressing epithelial cells. |
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V3314 | PTI-428 | 1953130-87-4 | PTI-428 is a novel, potent CFTR amplifier being developed byProteostasis Therapeutics, Inc. |
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V81689 | Urocortin III (mouse) (free acid) | Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (high affinity for CRF2 receptor). | |
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V74171 | Vanzacaftor | 2374124-49-7 | Vanzacaftor is a modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) used to study cystic fibrosis. |
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V74173 | Zatonacaftor | 2301945-38-8 | Zatonacaftor is a modulator of the cystic fibrosis transmembrane regulator (CFTR) protein. |
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