(R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933[1].
UCCF-853 is a CFTR modulator[1].
IOWH-032 is a novel and potent CFTR inhibitor (IC50=1.01 uM) in T84 and CHO-CFTR cell based assays.IC50 value: 1.01 uM (CHO-CFTR FLIPR) [1]Target: CFTRProfiling of iOWH032 showed it to be a CFTR inhibitor in T84 and CHO-CFTR cell based assays. It also demonstrated statistical significant inhibition at both 100 g & 10 g doses in the mouse closed-loop model. iOWH032 was further profiled in a cecetomized rat model. iOWH032 reduced the fecal output index by ~70%, compared to vehicle (choleratoxin), up to 8 hours after a single 5 mg/kg po dose.
Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF)[1].
Dirocaftor (PTI-808) is a CFTR potentiator that enhances the function of CFTR protein by opening chloride channels. Dirocaftor can be used for cystic fibrosis (CF) research[1][2].
(R)-Posenacaftor (R)-PTI-801) sodium is the R enantiomer of Posenacaftor. Posenacaftor is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF)[1].
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells[1].
Navocaftor, as a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, example 1)[1].
CFTR activator 1 is a potent and selective CFTR activator, with an EC50 of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease[1].
Lumacaftor (VX-809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
Glibenclamide (Glyburide) potassium is a potassium salt of Glibenclamide (HY-15206). Glibenclamid potassium exists in anhydrous and hydrate forms, with higher solubility compared to pure Glibenclamide[1].
CFTR corrector 11 (compound 133) is a CFTR corrector[1].
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research[1].
CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research[1].
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research[1].
Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
Zatonacaftor is a modulator of cystic fibrosis transmembrane regulator (CFTR) protein. Zatonacaftor can be used for research of cystic fibrosis[1][2].
VRT-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[1][2].
PTI-428 is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier[1].
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel[1][2].
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface[1][2].
(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)[1].
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
Aloisine 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[1][2].
CFTR 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[1].
(Rac)-Tezacaftor ((Rac)-VX-661) is a racemate of Tezacaftor (HY-15448). Tezacaftor is a F508del CFTR corrector. (Rac)-Tezacaftor can be used for the research of cystic fibrosis[1].