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CFTR

CFTR

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.

CFTR related products

Structure Cat No. Product Name CAS No. Product Description
(R)-Crinecerfont V96736 (R)-Crinecerfont 2649012-21-3 (R)-Crinecerfont is the R isomer of Crinecerfont.
(R)-Elexacaftor ((R)-VX-445) 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.
(R)-Olacaftor ((R)-VX-440) V74180 (R)-Olacaftor ((R)-VX-440) 1899111-41-1 (R)-Olacaftor ((R)-VX-440) is a cystic fibrosis transmembrane regulator (CFTR) modulator.
(R)-Posenacaftor sodium ((R)-PTI-801 sodium) V74181 (R)-Posenacaftor sodium ((R)-PTI-801 sodium) 2095064-09-6 (R)-Posenacaftor (R)-PTI-801) sodium is the R enantiomer of Posenacaftor.
(R)-Vanzacaftor ((R)-VX-121) V84845 (R)-Vanzacaftor ((R)-VX-121) 2374124-48-6
(Rac)-Tezacaftor ((Rac)-VX-661) V74179 (Rac)-Tezacaftor ((Rac)-VX-661) 1226709-85-8 (Rac)-Tezacaftor ((Rac)-VX-661) is the racemate of Tezacaftor.
6-PhEt-dATP V87142 6-PhEt-dATP 1239610-11-7 6-PhEt-dATP is an ATP analog that can specifically enhance the function of certain CFTR mutants and can be used in the study of cystic fibrosis.
Astressin 2B 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.
Astressin 2B TFA V85111 Astressin 2B TFA
Bamocaftor potassium (VX-659 potassium) V84403 Bamocaftor potassium (VX-659 potassium) 2204245-47-4 Bamocaftor potassium is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore F508del-CFTR protein function.
CFTR corrector 11 V74177 CFTR corrector 11 688050-45-5 CFTR corrector 11 (compound 133) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector.
CFTR corrector 12 V74164 CFTR corrector 12 958941-60-1 CFTR corrector 12 (compound 17C) is a bisthiazole analogue used as a CFTR corrector.
CFTR corrector 13 V99753 CFTR corrector 13 CFTR Corrector 13 (SVQ18) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector (EC50=3.14 μM).
CFTR corrector 14 V100334 CFTR corrector 14 CFTR corrector 14 (compound SVQ26) is a class 3 corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) that promotes CFTR activity (in the presence of the class C1 corrector VX-809, it increases CFTR activity with an EC50 of 3.08 μM).
CFTR corrector 15 V97850 CFTR corrector 15 1170387-92-4 CFTR Corrector 15 (Compound 4172) is a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) that, when combined with VX-809, can repair the F508del-CFTR folding defect.
CFTR corrector 16 V97466 CFTR corrector 16 1210305-23-9 CFTR calibrator 16 (Compound 39) is a calibrator of the cystic fibrosis transmembrane conductance regulator (CFTR) and can be used in the study of cystic fibrosis.
CFTR corrector 17 V93820 CFTR corrector 17 912790-04-6 CFTR Corrector 17 (Example 17) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator.
CFTR corrector 6 V74169 CFTR corrector 6 2226970-01-8 CFTR corrector 6 is a potent cystic fibrosis transmembrane conductance regulator (CFTR) enhancer.
CFTR corrector 8 V74176 CFTR corrector 8 1918142-35-4 CFTR corrector 8 is an efficient CFTR modulator.
CFTR potentiator 1 V87138 CFTR potentiator 1 CFTR potentiator 1 (I1421) is a potent CFTR potentiator with EC50 of 64 nM.
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