Guanylate-Cyclase-Activators-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html Guanylate HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html CyclaseGuanylate cyclase (guanylyl cyclase, GC), which catalyzes the formation of cGMP from GTP, exists in

2、 both the soluble and particulatefractions of cells. Guanylyl cyclases signal via the production of the second messenger cGMP.The GC family consists of particulate GC (pGC) and a nitric oxide-activated soluble GC (sGC). Seven pGC isoforms have yet beenfound (pGC-A to pGC-G). pGCs are activated by bi

3、nding of peptide ligands to their extracellular domains. sGC is a receptor forendogenous and exogenous nitric oxide and is activated several-fold upon its binding, constituting a core enzyme in the nitricoxide signal transduction pathway. cGMP generated by sGC is an important second messenger that r

4、egulates activity of severalenzymes triggering such important physiologic reactions as vasodilation, smooth muscle relaxation and platelet aggregation.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html Guanylate HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HY

5、PERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html Cyclase HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/

6、Guanylate Cyclase.html Agonists HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html & HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html HYPERLINK https:/www.MedChemE/Targets/Guanylate Cyclase.html Activators HYPERLINK h

7、ttps:/www.MedChemE/BM121307.html (4-Acetamidocyclohexyl) HYPERLINK https:/www.MedChemE/BM121307.html HYPERLINK https:/www.MedChemE/BM121307.html nitrate(BM121307) Cat. No.: HY-100295 HYPERLINK https:/www.MedChemE/rac-bi-703704.html (Rac)-BI HYPERLINK https:/www.MedChemE/rac-bi-703704.html HYPERLINK

8、https:/www.MedChemE/rac-bi-703704.html 703704Cat. No.: HY-117962(4-Acetamidocyclohexyl) nitrate (BM121307) is aguanylate cyclase activator.(Rac)-BI 703704 is a potent soluble guanylylcyclase (sGC) activator. (Rac)-BI 703704 reducesprogression of renal damage in the ZSF1 rat, andhighlight the potenti

9、al of sGC activation as aneffective therapy for diabetic nephropathy.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/rac-mgv354.html (Rac)-MGV354Cat. No.: HY-117917 HYPERLINK https:/www.M

10、edChemE/ataciguat.html Ataciguat(HMR-1766) Cat. No.: HY-17500(Rac)-MGV354 is the racemate of MGV354. MGV354 isa soluble guanylate cyclase (sGC) activator withEC s of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK h

11、ttps:/www.MedChemE/cfm-1571-hydrochloride.html CFM HYPERLINK https:/www.MedChemE/cfm-1571-hydrochloride.html HYPERLINK https:/www.MedChemE/cfm-1571-hydrochloride.html 1571 HYPERLINK https:/www.MedChemE/cfm-1571-hydrochloride.html HYPERLINK https:/www.MedChemE/cfm-1571-hydrochloride.html hydrochlorid

12、e HYPERLINK https:/www.MedChemE/cfm-1571-hydrochloride.html HYPERLINK https:/www.MedChemE/Cinaciguat.html CinaciguatCat. No.: HY-107546(BAY 58-2667) Cat. No.: HY-14181CFM 1571 hydrochloride is the stimulator of thenitric oxide receptor, soluble guanylate cyclase(sGC) with an EC50 and IC50 of 5.49 M

13、and 2.84M, respectively. Soluble guanylate cyclase (sGC)is a key signal-transduction enzyme activated bynitric oxide (NO).Cinaciguat is an activator of guanylate cyclase(sGC), and used for acute decompensated heartfailure.Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99

14、.20%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Cinaciguat-hydrochloride.html Cinaciguat HYPERLINK https:/www.MedChemE/Cinaciguat-hydrochloride.html HYPERLINK https:/www.MedChemE/Cinaciguat-h

15、ydrochloride.html hydrochloride(BAY 58-2667 hydrochloride) Cat. No.: HY-14181A HYPERLINK https:/www.MedChemE/ebselen-oxide.html Ebselen HYPERLINK https:/www.MedChemE/ebselen-oxide.html HYPERLINK https:/www.MedChemE/ebselen-oxide.html oxideCat. No.: HY-114548Cinaciguat hydrochloride is a potent solub

16、leguanylate cyclase (GC) activator with EC of 1550nM in platelets.Ebselen oxide, the selenone analogue of Ebselen,covalently modifies diguanylate cyclase (DGC) toinhibit c-di-GMP-receptor interactions and reducesDGC activity. Ebselen oxide also inhibits alginateproduction (IC =14 M) by50 Pseudomonas

17、aeruginosa.Purity: 99.52%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/guanylate-cyclase-in-1.html Guanylate HYPERLINK https:/www.MedChemE/guanylate-cyclase-in-1.html HYPERLINK https:/ww

18、w.MedChemE/guanylate-cyclase-in-1.html cyclase-IN-1 HYPERLINK https:/www.MedChemE/guanylate-cyclase-in-1.html HYPERLINK https:/www.MedChemE/guanylin-human.html Guanylin(human)Cat. No.: HY-W021162 Cat. No.: HY-P1179Guanylate cyclase-IN-1 (Example 46) is a guanylatecyclase inhibitor that can be used f

19、orcardiovascular diseases research.Guanylin(human), a 15-amino acid peptide, is anendogenous intestinal guanylate cyclase activator.Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/guany

20、lin-human-tfa.html Guanylin(human) HYPERLINK https:/www.MedChemE/guanylin-human-tfa.html HYPERLINK https:/www.MedChemE/guanylin-human-tfa.html TFACat. No.: HY-P1179A HYPERLINK https:/www.MedChemE/Lificiguat.html Lificiguat(YC-1) Cat. No.: HY-14927Guanylin(human) TFA, a 15-amino acid peptide, isan en

21、dogenous intestinal guanylate cyclaseactivator.Lificiguat binds to the subunit of solubleguanylyl cyclase(sGC) with K of 0.6-1.1 M indthe presence of CO.Purity: 97.45%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

22、mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/Linaclotide.html Linaclotide HYPERLINK https:/www.MedChemE/Linaclotide.html HYPERLINK https:/www.MedChemE/ly83583.html LY83583Cat. No.: HY-17584 Cat. No.: HY-W013386Linaclotide is a potent and selective guanylatecyclase C agonist; developed for

23、 the treatment ofconstipation-predominant irritable bowel syndrome(IBS-C) and chronic constipation.LY83583 is a cell-permeable and competitiveinhibitor of soluble guanylate cyclase (sGC) withan IC value of 2 M.50Purity: 98.44%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical Da

24、ta: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Methylene-Blue.html Methylene HYPERLINK https:/www.MedChemE/Methylene-Blue.html HYPERLINK https:/www.MedChemE/Methylene-Blue.html Blue HYPERLINK https:/www.MedChemE/Methylene-Blue.html HYPERLINK https:/www.MedChemE/methylene-b

25、lue-trihydrate.html Methylene HYPERLINK https:/www.MedChemE/methylene-blue-trihydrate.html HYPERLINK https:/www.MedChemE/methylene-blue-trihydrate.html blue HYPERLINK https:/www.MedChemE/methylene-blue-trihydrate.html HYPERLINK https:/www.MedChemE/methylene-blue-trihydrate.html trihydrate(Basic Blue

26、 9; CI-52015; Methylthioninium chloride) Cat. No.: HY-14536 (C.I. Basic Blue 9 trihydrate) Cat. No.: HY-B1359Methylene blue (Basic Blue 9) is a guanylyl cyclase(sGC), monoamine oxidase A (MAO-A) and NOsynthase (NOS) inhibitor. Methylene blue is avasopressor and is often used as a dye in severalmedic

27、al procedures.Methylene blue trihydrate (C.I. Basic Blue 9trihydrate) is a guanylyl cyclase (sGC),monoamine oxidase A (MAO-A) and NO synthase(NOS) inhibitor. Methylene blue trihydrate is avasopressor and is often used as a dye in severalmedical procedures.Purity: 98.0%Clinical Data: LaunchedSize: 10

28、0 mg, 500 mgPurity: 97.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/sGC_activator_1.html MGV354 HYPERLINK https:/www.MedChemE/sGC_activator_1.html HYPERLINK https:/www.MedChemE/mm-419447.html MM HYPERLINK https:/www.MedChemE/mm-419447.html HYP

29、ERLINK https:/www.MedChemE/mm-419447.html 419447Cat. No.: HY-111516 Cat. No.: HY-P3282MGV354 is a soluble guanylate cyclase (sGC)activator with EC s of 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

30、, 10 mg HYPERLINK https:/www.MedChemE/mosliciguat.html MosliciguatCat. No.: HY-137446 HYPERLINK https:/www.MedChemE/Nelociguat.html Nelociguat(BAY60-4552) Cat. No.: HY-78237Mosliciguat is a guanylate cyclase activator.Nelociguat (BAY60-4552) is a nitric oxidesensitive soluble guanylate cyclase stimu

31、lator.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.73%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/ns-2028.html NS-2028 HYPERLINK https:/www.MedChemE/ns-2028.html HYPERLINK https:/www.MedChemE/odq.html ODQCat.

32、 No.: HY-12379 Cat. No.: HY-101255NS-2028 is a highly selective soluble GuanylylCyclase (sGC) inhibitor with IC values of 30 nM50and 200 nM for basal and NO-stimulated enzymeactivity.ODQ is a potent and selective soluble guanylylcyclase (sGC, nitric oxide-activated enzyme)inhibitor. ODQ enhances the

33、 pro-apoptotic effectsof Cisplatin in human mesothelioma cells.Purity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.52%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/olinciguat.html Olinc

34、iguat HYPERLINK https:/www.MedChemE/olinciguat.html HYPERLINK https:/www.MedChemE/plecanatide.html Plecanatide(IW-1701) Cat. No.: HY-109066Cat. No.: HY-108741Olinciguat (IW-1701) is an oral guanylate cyclase(sGC) stimulator with concentration-dependentstimulation of sGC in purified rat and humanenzy

35、me assays and a whole cell assay.Plecanatide, an analogue of Uroguanylin, is anorally active guanylate cyclase-C (GC-C) receptoragonist. Plecanatide activates GC-C receptors tostimulate cGMP synthesis with an EC of 190 nM50in T84 cells assay.Purity: 98.44%Clinical Data: No Development ReportedSize:

36、5 mg, 10 mg, 50 mg, 100 mgPurity: 98.90%Clinical Data: LaunchedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Plecanatide_acetate.html Plecanatide HYPERLINK https:/www.MedChemE/Plecanatide_acetate.html HYPERLINK https:/www.MedChemE/Plecanatide_acetate.html acetate HYPERLINK https:/www.MedChemE/Plec

37、anatide_acetate.html HYPERLINK https:/www.MedChemE/praliciguat.html PraliciguatCat. No.: HY-108741A(IW-1973) Cat. No.: HY-109039Plecanatide acetate, an analogue of Uroguanylin,is an orally active guanylate cyclase-C (GC-C)receptor agonist. Plecanatide acetate activatesGC-C receptors to stimulate cGM

38、P synthesis with anEC of 190 nM in T84 cells assay.50Praliciguat (IW-1973) is a potent and orallyactive soluble guanylate cyclase stimulator,enhances NO signaling, acts as a vasodilator.Praliciguat (IW-1973) stimulates sGC in HEK-293cells with an EC of 197 nM.50Purity: 99.26%Clinical Data: LaunchedS

39、ize: 5 mg, 10 mgPurity: 98.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Riociguat.html Riociguat(BAY 632521) Cat. No.: HY-14779 HYPERLINK https:/www.MedChemE/riociguat-13c

40、-d3.html Riociguat-13C-d3(BAY 632521-13C-d3) Cat. No.: HY-14779S2Riociguat is an oral stimulator of solubleguanylate cyclase (sGC) used in the treatment ofpulmonary hypertension.Riociguat-13C-d3 (BAY 632521-13C-d3) is the 13C-and deuterium labeled Riociguat. Riociguat is anoral stimulator of soluble guanylate cyclase(sGC) used in the treatment of pulmonaryhypertension.Purity: 99.58%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/riocig