CFTR
Cystic fibrosis transmembrane conductance regulator
CFTR (Cystic fibrosis transmembrane conductance regulator), mutations of which cause cystic fibrosis, belongs to the ATP-binding cassette (ABC) transporter family and works as a channel for small anions, such as chloride and bicarbonate. CFTR is composed of two homologous halves, each comprising a transmembrane (TMD) and a nucleotide binding domain (NBD). CFTR activity is regulated by phosphorylation of its cytosolic regulatory (R) domain, and ATP binding and hydrolysis at two NBDs.
CFTR is expressed in many cell types throughout the body, but in the airways it is found mainly in secretory serous cells of the submucosal glands. Transitions between open and closed states of CFTR are regulated by ATP binding and hydrolysis on the cytosolic nucleotide binding domains, which are coupled with the transmembrane (TM) domains forming the pathway for anion permeation. CFTR function is normally tightly controlled as dysregulation can lead to life-threatening diseases such as secretory diarrhoea and cystic fibrosis.
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CFTR Related Products (134)
Related Products (134)
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Antibodies (1)
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CFTR corrector 14
0 ImagesCat. No.: HY-161895CFTR corrector 14 (Compound SVQ26) is a class 3 corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that promotes the CFTR activity (EC50 of 3.08 μM with presence of C1 class corrector VX-809). CFTR corrector 14 regulates the mutant-caused misfolding and impaired function of the CFTR protein. CFTR corrector 14 can be used in research about cystic fibrosis.
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Riselcaftor
0 ImagesCat. No.: HY-164037CAS No.: 2799652-36-9Riselcaftor (Example 33) is a CFTR modulator, with an EC50 of 20.1 nM in human bronchial epithelial cells. Riselcaftor can be used for research of cystic fibrosis.
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GLPG2737
0 ImagesCat. No.: HY-158144CAS No.: 2093974-63-9GLPG2737 is a potent CFTR type 2 corrector, and GLPG2737 can be used in combination with a type 1 co-corrector in the study of cystic fibrosis.
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Aloisine A
0 ImagesCat. No.: HY-112363CAS No.: 496864-16-5Synonyms: RP107Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
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VRT-532
0 ImagesSynonyms: CFpot-532VRT-532 (CFpot-532) is a potent is a potent CFTR modulator. VRT-532 enhances channel activity in G551D-CFTR and intrinsic ATPase activity of G551D-CFTR. VRT-532 has the potential for the research of cystic fibrosis.
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CFTR corrector 13
0 ImagesCat. No.: HY-161894CFTR corrector 13 (SVQ18) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector (EC50=3.14 μM). CFTR corrector 13 enhances the function of CFTR channels, especially when used in combination with Lumacaftor (HY-13262), it can produce a dose-dependent increase in CFTR function. CFTR corrector 13 can be used in the study of cystic fibrosis (CF) and other CFTR-related diseases.
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Glibenclamide (Standard)
0 ImagesSynonyms: Glyburide (Standard)Glibenclamide (Standard) is the analytical standard of Glibenclamide. This product is intended for research and analytical applications. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
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CFTR corrector 18
0 ImagesCat. No.: HY-172555CAS No.: 2993441-49-7CFTR corrector 18 (Compound I-99) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 18 facilitates the processing and trafficking of CFTR, increasing the number of CFTR on the cell surface. CFTR corrector 18 is promising for research of cystic fibrosis (CF).
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CRF1 receptor antagonist-1
0 ImagesCat. No.: HY-156522CAS No.: 2635364-30-4CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH).
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(R)-Olacaftor
0 ImagesSynonyms: (R)-VX-440(R)-Olacaftor ((R)-VX-440) is a Cystic fibrosis transmembrane conductance regulator (CFTR) modulator. (R)-Olacaftor has good potential for the study of cystic fibrosis (CF).
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VU439
0 ImagesCat. No.: HY-174821VU439 is a functionalized photoaffinity ligand of Elexacaftor (HY-111772). VU439 retains the activity of Elexacaftor as a CFTR corrector and can identify SCCPDH as a specific off-target of Elexacaftor through chemoproteomics.
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(R)-Crinecerfont
0 ImagesCat. No.: HY-106203BCAS No.: 2649012-21-3Synonyms: (R)-SSR-125543(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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CFTR corrector 9
0 ImagesCFTR corrector 9 (compound 42) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator. CFTR corrector 9 can be used for researching cystic fibrosis (CF) and other CFTR associated disorders.
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MS5128
0 ImagesCat. No.: HY-183725CAS No.: 3060520-82-0MS5128 is an OTUB1-based deubiquitinase-targeting chimera (DUBTAC) targeting CFTR. MS5128 recruits OTUB1 to CFTR to induce deubiquitination and stabilization of CFTR. MS5128 can be used for the research of cystic fibrosis. (Blue: CFTR Ligand (HY-183724); Pink: OTUB1 Ligand (HY-13262); Black: Linker)
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Crinecerfont tosylate
0 ImagesCat. No.: HY-106203CCAS No.: 2649012-17-7Synonyms: SSR-125543 tosylateCrinecerfont (SSR-125543) tosylate is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont tosylate blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont tosylate improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont tosylate can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. Crinecerfont tosylate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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(R)-Vanzacaftor-d4
0 ImagesCat. No.: HY-145603ASSynonyms: (R)-VX-121-d4(R)-Vanzacaftor-d4 ((R)-VX-121-d4) is the deuterated-labeled (R)-Vanzacaftor (HY-145603A). (R)-Vanzacaftor ((R)-VX-121) is a Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) modulator with max activity of 30-60% and EC50 of <1 μM in enteroid cells. (R)-Vanzacaftor can be used for the research of cystic fibrosis.
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MS6178
0 ImagesCat. No.: HY-185122CAS No.: 3060520-53-5
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AF-2785
0 ImagesCat. No.: HY-116806CAS No.: 252025-48-2AF-2785 is a potent CFTR blocker. AF-2785 inhibits the cAMP-activated chloride current in rat epididymal cells with an IC50 of 170.6 μM. AF-2785 can be used in research related to contraceptives.
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AAG561
0 ImagesCat. No.: HY-177313CAS No.: 235760-14-2Synonyms: NVP-AAG 561AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. AAG561 can be used for the study of the underlying emotion dysregulation of a mental disease or disorder.
