CFTR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/CFTR.html CFTRCystic fibrosis transmembrane conductance regulatorCFTR (Cystic fibrosis transmembrane conductance regulator), mutations of which cause cystic fibrosis, belongs to the ATP-bindingcassette (ABC) transporter family and works as a channel for small a

2、nions, such as chloride and bicarbonate. CFTR is composed oftwo homologous halves, each comprising a transmembrane (TMD) and a nucleotide binding domain (NBD). CFTR activity isregulated by phosphorylation of its cytosolic regulatory (R) domain, and ATP binding and hydrolysis at two NBDs.CFTR is expr

3、essed in many cell types throughout the body, but in the airways it is found mainly in secretory serous cells of thesubmucosal glands. Transitions between open and closed states of CFTR are regulated by ATP binding and hydrolysis on thecytosolic nucleotide binding domains, which are coupled with the

4、 transmembrane (TM) domains forming the pathway for anionpermeation. CFTR function is normally tightly controlled as dysregulation can lead to life-threatening diseases such as secretorydiarrhoea and cystic fibrosis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/CFTR.html CFTR HYPERLINK https:

5、/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CFTR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CFTR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CFTR.html Antago

6、nists, HYPERLINK https:/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CFTR.html Activators HYPERLINK https:/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CFTR.html & HYPERLINK https:/www.MedChemE/Targets/CFTR.html HYPERLINK https:/www.MedChemE/Targets/CF

7、TR.html Modulators HYPERLINK https:/www.MedChemE/_R_-BPO-27.html (R)-BPO-27Cat. No.: HY-19778 HYPERLINK https:/www.MedChemE/r-posenacaftor-sodium.html (R)-Posenacaftor HYPERLINK https:/www.MedChemE/r-posenacaftor-sodium.html HYPERLINK https:/www.MedChemE/r-posenacaftor-sodium.html sodium(R)-PTI-801

8、sodium) Cat. No.: HY-109187B(R)-BPO-27, the R enantiomer of BPO-27, is apotent, orally active and ATP-competitiveCFTR inhibitor with an IC of 4 nM.50(R)-Posenacaftor (R)-PTI-801) sodium is the Renantiomer of Posenacaftor. Posenacaftor is acystic fibrosis transmembrane regulator (CFTR)protein modulat

9、or that corrects the folding andtrafficking of CFTR protein.Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/aloisine-a.html Alo

10、isine HYPERLINK https:/www.MedChemE/aloisine-a.html HYPERLINK https:/www.MedChemE/aloisine-a.html A(RP107) Cat. No.: HY-112363 HYPERLINK https:/www.MedChemE/PTC124.html Ataluren(PTC124) Cat. No.: HY-14832Aloisine A (RP107) is a a potent cyclin-dependentkinase (CDK) inhibitor with IC s of 0.15 M, 0.1

11、250M, 0.4 M, 0.16 M for CDK1/cyclin B, CDK2/cyclinA, CDK2/cyclin E, CDK5/p35, respectively. AloisineA ininhibits GSK-3 (IC =0.5 M) and GSK-350(IC =1.5 M).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgAtaluren (PTC124) is an orally availableCFTR-G542X nonsense allele inhibitor.Pu

12、rity: 99.71%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/bamocaftor.html Bamocaftor(VX-659) Cat. No.: HY-126394 HYPERLINK https:/www.MedChemE/BPO-27-racemate.html BPO-27 HYPERLINK https:/www.MedChemE/BPO-27-racemate.html HYPERLINK https:/www.Med

13、ChemE/BPO-27-racemate.html racemateCat. No.: HY-19778ABamocaftor (VX-659) is a cystic fibrosistransmembrane conductance regulator (CFTR)corrector designed to restore F508del-CFTR proteinfunction. Bamocaftor can be used combine withTezacaftor and Ivacaftor in cystic fibrosisresearch.BPO-27 racemate i

14、s a potent CFTR inhibitor withan IC of 8 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 50 mg, 100 mg, 200 mgPurity: 98.37%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cavosonstat.html Cavosonstat HYPERLINK https:/www.MedChemE/cavosonstat.h

15、tml HYPERLINK https:/www.MedChemE/cftr-corrector-2.html CFTR HYPERLINK https:/www.MedChemE/cftr-corrector-2.html HYPERLINK https:/www.MedChemE/cftr-corrector-2.html corrector HYPERLINK https:/www.MedChemE/cftr-corrector-2.html HYPERLINK https:/www.MedChemE/cftr-corrector-2.html 2(N91115) Cat. No.: H

16、Y-109027Cat. No.: HY-125381Cavosonstat (N91115) is an orally activeS-nitrosoglutathione reductase (GSNOR) inhibitor.Cavosonstat is a CFTR stabilizer, and can be usedfor cystic fibrosis research.CFTR corrector 2 is a cystic fibrosis transmembraneconductance corrector (CFTR), extracted frompatent US20

17、140274933.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.29%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cftr-corrector-4.html CFTR HYPERLINK https:/www.MedChemE/cftr-corrector-4.html HYPERLINK https:/www.Med

18、ChemE/cftr-corrector-4.html corrector HYPERLINK https:/www.MedChemE/cftr-corrector-4.html HYPERLINK https:/www.MedChemE/cftr-corrector-4.html 4 HYPERLINK https:/www.MedChemE/cftr-corrector-4.html HYPERLINK https:/www.MedChemE/cftr-corrector-6.html CFTR HYPERLINK https:/www.MedChemE/cftr-corrector-6.

19、html HYPERLINK https:/www.MedChemE/cftr-corrector-6.html corrector HYPERLINK https:/www.MedChemE/cftr-corrector-6.html HYPERLINK https:/www.MedChemE/cftr-corrector-6.html 6Cat. No.: HY-135279 Cat. No.: HY-136939CFTR corrector 4 (Compound 13), an active(R,R)-form enantiomer, is a highly potent andora

20、lly active cystic fibrosis transmembraneconductance regulator (CFTR) corrector.CFTR corrector 6 is a potent potentiator of CysticFibrosis Transmembrane conductance Regulator(CFTR). CFTR corrector 6 has the potential forcystic fibrosis (CF) and other CFTR associateddisorders research.Purity: 98%Clini

21、cal Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.87%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/CFTR_inh_-172.html CFTR(inh)-172 HYPERLINK https:/www.MedChemE/CFTR_inh

22、_-172.html HYPERLINK https:/www.MedChemE/chromanol-293b.html Chromanol HYPERLINK https:/www.MedChemE/chromanol-293b.html HYPERLINK https:/www.MedChemE/chromanol-293b.html 293BCat. No.: HY-16671 Cat. No.: HY-108575CFTR(inh)-172 is a potent and selective blocker ofthe CFTR chloride channel; reversibly

23、 inhibitsCFTR short-circuit current in less than 2 minuteswith a K of 300 nM.iChromanol 293B is a selective blocker of theslow delayed rectifier K+ current (IKs) withIC50 of 1-10 M and a weak inhibitor of KATPchannel. Chromanol 293B also blocks the CFTRchloride current with an IC of 19 M.50Purity: 9

24、8.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cp-628006.html CP-628006Cat. No.: HY-145126 HYPERLINK https:/www.MedChemE/crinecerfont.html Crinecerfont(SSR-125543) Cat. No.

25、: HY-106203CP-628006, a small molecule CFTR potentiator,restores ATP-dependent channel gating to thecystic fibrosis mutant G551D-CFTR.Crinecerfont (SSR-125543) hydrochloride is apotent, orally active, non-peptide CRF1 receptorantagonist. Crinecerfont can be used for Classiccongenital adrenal hyperpl

26、asia (CAH) research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/crinecerfont-hydrochloride.html Crinecerfont HYPERLINK https:/www.MedChemE/crinecerfont-hydrochloride.html HYPERLINK ht

27、tps:/www.MedChemE/crinecerfont-hydrochloride.html hydrochloride(SSR-125543 hydrochloride; SSR-125543A) Cat. No.: HY-106203A HYPERLINK https:/www.MedChemE/dirocaftor.html Dirocaftor(PTI-808) Cat. No.: HY-137437Crinecerfont (SSR-125543) hydrochloride is apotent, orally active, non-peptide CRF1 recepto

28、rantagonist. Crinecerfont can be used for Classiccongenital adrenal hyperplasia (CAH) research.Dirocaftor (PTI-808) is a CFTR potentiator thatenhances the function of CFTR protein by openingchloride channels. Dirocaftor can be used forcystic fibrosis (CF) research.Purity: 98%Clinical Data: No Develo

29、pment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cftr-corrector-1.html Elexacaftor HYPERLINK https:/www.MedChemE/cftr-corrector-1.html HYPERLINK https:/www.MedChemE/galicaftor.html Galicaftor(VX-445)

30、Cat. No.: HY-111772 (ABBV-2222; GLPG-2222) Cat. No.: HY-111111Elexacaftor (VX-445, Compound 1) is a modulator ofcystic fibrosis transmembrane conductance regulator(CFTR). Elexacaftor (VX-445, Compound 1)facilitates the processing and trafficking of CFTRto increase the amount of CFTR at the cellsurfa

31、ce.Galicaftor (ABBV-2222; GLPG-2222) is a potent andorally active cystic fibrosis transmembraneconductance regulator (CFTR) corrector.Galicaftor can be used for cystic fibrosisresearch.Purity: 99.50%Clinical Data: LaunchedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Develop

32、ment ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/glibenclamide.html Glibenclamide HYPERLINK https:/www.MedChemE/glibenclamide.html HYPERLINK https:/www.MedChemE/glpg-3221.html GLPG-3221(Glyburide) Cat. No.: HY-15206Cat. No.: HY-133013Glibenclamide (Glyburide) is an orally activeATP-sensi

33、tive K+ channel (K ) inhibitor andATPcan be used for the research of diabetes andobesity. Glibenclamide inhibits P-glycoprotein.GLPG-3221 is a potent, orally active corrector ofCFTR (cystic fibrosis transmembrane conductanceregulator), with an EC of 105 nM. GLPG-322150can be uesd for the treatment o

34、f cystic fibrosis.Purity: 99.79%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/GLPG1837.html GLPG1837(ABBV-974) Cat. No.: HY-111099 HYPERLINK https:/www.MedChemE/glpg2451.html GLPG

35、2451Cat. No.: HY-119936GLPG1837 is a potent and reversible CFTRpotentiator, with EC s of 3 nM and 339 nM for50F508del and G551D CFTR, respectively.GLPG2451 is a cystic fibrosis transmembraneconductance regulator (CFTR) potentiator, whicheffectively potentiates low temperature rescuedF508del CFTR wit

36、h an EC of 11.1 nM.50Purity: 99.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/glyburide-d11.html Glyburide-d11Cat. No.: HY-15206

37、S HYPERLINK https:/www.MedChemE/glyburide-d3.html Glyburide-d3(Glyburide-d3) Cat. No.: HY-15206S1Glyburide-d11 is the deuterium labeledGlibenclamide. Glibenclamide (Glyburide) is anorally active ATP-sensitive K+ channel (K )ATPinhibitor and can be used for the research ofdiabetes and obesity. Gliben

38、clamide inhibitsP-glycoprotein.Glyburide-d3 (Glyburide-d3) is the deuteriumlabeled Glibenclamide. Glibenclamide (Glyburide)is an orally active ATP-sensitive K+ channel(K ) inhibitor and can be used for theATPresearch of diabetes and obesity. Glibenclamideinhibits P-glycoprotein.Purity: 98%Clinical D

39、ata: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/GlyH-101.html GlyH-101Cat. No.: HY-18336 HYPERLINK https:/www.MedChemE/icenticaftor.html Icenticaftor(QBW251) Cat. No.: HY-109177GlyH-101 is a cell-permeable g

40、lycinyl hydrazonecompound that blocks CFTR with Ki of 1.4 uM. IC50value: 1.4 uM (Ki, at +60 mV) Target: CFTR invitro: GlyH-101 reversibly inhibited CFTR Cl-conductance in 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909

41、 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ivacaftor-d19.html Ivacaftor-d19(VX-770-d19) Cat. No.: HY-13017S1 HYPERLINK https:/www.MedChemE/ivacaftor-d9.html Ivacaftor-d9(VX-770-d9) Cat. No.: HY-13017SIvacaftor-d19 (VX-770-d19) is the deuteriumlabeled Ivacaftor. Ivacaftor (VX-770) is a poten

42、tand orally bioavailable CFTR potentiator,targeting G551D-CFTR and F508del-CFTR with EC s50of 100 nM and 25 nM, respectively.Ivacaftor-D9 (CTP-656) is a potent CFTRmodulator and exhibits an EC value of 25550nM for CFTR potentiation in G551D/F508del HBECells. Ivacaftor-D9 acts as an orally active and

43、improved deuterated Ivacaftor analog for cysticfibrosis research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/k41498-tfa.html K41498 HYPERLINK https:/www.MedChemE/k41498-tfa.html HYPERLINK https:/www

44、.MedChemE/k41498-tfa.html TFA HYPERLINK https:/www.MedChemE/k41498-tfa.html HYPERLINK https:/www.MedChemE/KM11060.html KM11060Cat. No.: HY-P1106A Cat. No.: HY-19970K41498 TFA is a potent and highly selectiveCRF2 receptor antagonist with K valuesiof 0.66 nM, 0.62 nM and 425 nM for human CRF ,2CRF and

45、 CRF receptors respectively.2 1KM11060 is a corrector of the F508 deletion(F508del)-cystic fibrosis transmembraneconductance regulator (CFTR) trafficking defect.KM11060 can be used for the research ofF508del-CFTR processing defect and development ofcystic fibrosis therapeutics.Purity: 98%Clinical Da

46、ta: No Development ReportedSize: 1 mg, 5 mgPurity: 99.59%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/kobusin.html KobusinCat. No.: HY-N5101 HYPERLINK https:/www.MedChemE/VX-809.html Lumacaftor(VX-809; VRT 826809) Cat. No.: HY-1326

47、2Kobusin is a bisepoxylignan isolated from thePnonobio biondii Pamp. Kobusin is an activatorof CFTR and CaCCgie chloride channels and ainhibitor of ANO1/CaCC (calcium-activatedchloride channel) channel.Lumacaftor (VX-809; VRT 826809) is a CFTRmodulator that corrects the folding andtrafficking of CFT

48、R protein.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.19%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/navocaftor.html Navocaftor HYPERLINK https:/www.MedChemE/navocaftor.html HYPERLINK https:/www.MedChemE/PT

49、I-428.html Nesolicaftor(GLPG 3067; ABBV-3067) Cat. No.: HY-109152 (PTI-428) Cat. No.: HY-111680Navocaftor (GLPG 3067), as a cystic fibrosistransmembrane regulator (CFTR), is a proteinmodulator (US 20200377491 Al, example 1).Nesolicaftor (PTI-428) is a specific cysticfibrosis transmembrane conductanc

50、e regulator(CFTR) amplifier.Purity: 99.05%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.65%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/njh-2-057.html NJH-2-057 HYPERLINK https:/www.MedChemE/njh-2-057.html

51、HYPERLINK https:/www.MedChemE/CFTR_corrector.html OlacaftorCat. No.: HY-115878(VX-440) Cat. No.: HY-112267NJH-2-057 is an EN523 OTUB1 recruiter linked tolumacaftor, a drug used to treat cystic fibrosisthat binds F508-CFTR.Olacaftor (VX-440) is a cystic fibrosistransmembrane conductance regulator (CF

52、TR)modulator extracted from patent US9782408.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/pg01.html PG01Cat. No.: HY-103369 HYPERLINK https:/www.MedChemE/posenacaftor.ht

53、ml Posenacaftor(PTI-801) Cat. No.: HY-109187PG01 is a potent CFTR Cl- channel potentiator.PG01 can correct gating defects of CFTR mutants,is effective on bE193K, G970R and G551D(CFTR mutants) with K values of 0.22 M, 0.45dM and 1.94 M, respectively. PG01 is alsoeffective on F508 (K of 0.3 M).aPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPosenacaftor (PTI-801) is a cystic