PGE-synthase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html PGE HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html synthaseProstaglandin E synthasePGE synthase (Prostaglandin E synthase), which converts cyclooxygenase (COX)-derived prostaglan

2、din H (PGH ) to PGE , is known2 2 2to comprise a group of at least three structurally and biologically distinct enzymes. There are membrane-associated PGES(mPGES)-1, mPGES-2, and cytosolic PGES (cPGES).mPGES-1 is a perinuclear protein that is markedly induced by proinflammatory stimuli and downregul

3、ated by anti-inflammatoryglucocorticoids as in the case of COX-2. It is functionally coupled with COX-2 in marked preference to COX-1. mPGES-2 issynthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads tothe formation of a mature cyto

4、solic enzyme. This enzyme is rather constitutively expressed in various cells and tissues and isfunctionally coupled with both COX-1 and COX-2. cPGES is constitutively expressed in a wide variety of cells and is functionally linked to COX-1 to promote immediate PGE production.2www.MedChemE 1 HYPERLI

5、NK https:/www.MedChemE/Targets/PGE synthase.html PGE HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html synthase HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html Inhibitors HYP

6、ERLINK https:/www.MedChemE/Targets/PGE synthase.html HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html & HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html HYPERLINK https:/www.MedChemE/Targets/PGE synthase.html Agonists HYPERLINK https:/www.MedChemE/s-flurbiprofen.html (S)-Flurbiprofen(E

7、sflurbiprofen) Cat. No.: HY-15123 HYPERLINK https:/www.MedChemE/s-flurbiprofen-d3.html (S)-Flurbiprofen-d3(Esflurbiprofen-d3) Cat. No.: HY-15123S(S)-Flurbiprofen is an active enantiomer ofFlurbiprofen, with IC values of 0.48 M and 0.4750M for COX-1 and COX-2, respectively.(S)-Flurbiprofen-d3 (Esflur

8、biprofen-d3) is thedeuterium labeled (S)-Flurbiprofen.(S)-Flurbiprofen is an active enantiomer ofFlurbiprofen, with IC values of 0.48 M and 0.4750M for COX-1 and COX-2, respectively.Purity: 99.83%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 250 mg, 500 mgPurity: 98%Clinical Data: No Development

9、ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/at-56.html AT-56 HYPERLINK https:/www.MedChemE/at-56.html HYPERLINK https:/www.MedChemE/Benzydamine-hydrochloride.html Benzydamine HYPERLINK https:/www.MedChemE/Benzydamine-hydrochloride.html HYPERLINK https:/www.MedChemE/Benzydamine-hydrochlori

10、de.html hydrochlorideCat. No.: HY-13988 Cat. No.: HY-30235AAT-56 is a potent, selective and orally activeinhibitor of lipocalin-type prostaglandin Dsynthase (L-PGDS) IC50 Ki, with an of 95 M andof 75 M. AT-56 could selectively suppress thedrowsiness or pain reaction mediated byL-PGDS-catalyzed PGD .

11、2Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgBenzydamine hydrochloride is a locally-actingnonsteroidal anti-inflammatory drug with localanaesthetic and analgesic properties; selectivelybinds to prostaglandin synthetase and has notablein vitro antibacterial activity.Purit

12、y: 98.02%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/Bismuth-Subsalicylate.html Bismuth HYPERLINK https:/www.MedChemE/Bismuth-Subsalicylate.html HYPERLINK https:/www.MedChemE/Bismuth-Subsalicylate.html Subsalicylate(Bismuth oxysalicylate; Bismuth(III) salicylate bas

13、ic) Cat. No.: HY-B0550 HYPERLINK https:/www.MedChemE/brp-201.html BRP-201Cat. No.: HY-144237Bismuth Subsalicylate is a potent and orallyactive antacid and anti-diarrheal agent. BismuthSubsalicylate reduces inflammation/irritation ofstomach and intestinal lining through inhibitionof prostaglandin syn

14、thesis in vivo.Brp-201 is considered as a promising therapeutictarget for the next generation ofanti-inflammatory drugs in the treatment ofinflammatory diseases. It is a new, effective andselective inhibitor of mPGES-1 with an IC value50of 0.42 M.Purity: 98%Clinical Data: LaunchedSize: 500 mg, 5 g,

15、10 gPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cafestol.html Cafestol HYPERLINK https:/www.MedChemE/cafestol.html HYPERLINK https:/www.MedChemE/cay10526.html CAY10526Cat. No.: HY-N6257 Cat. No.: HY-118119Cafestol, one of the major components of co

16、ffee,is a coffee-specific diterpene from. Cafestol is aERK inhibitor for AP-1-targeted activity againstPGE production and the mRNA expression of2cyclooxygenase (COX)-2 in LPS-activated RAW264.7cells.CAY10526 is a specific microsomal PGE2 synthase-1(mPGES1) inhibitor. CAY10526 inhibits PGE2production

17、 through the selective modulation ofmPGES1 expression but does not affect COX-2.Purity: 99.91%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/clopirac.html Clopirac HYPERLINK https:/www.MedC

18、hemE/clopirac.html HYPERLINK https:/www.MedChemE/dehydroevodiamine.html DehydroevodiamineCat. No.: HY-W173220 Cat. No.: HY-N2106Clopirac is a potent and orally active inhibitorof prostaglandin synthetase. Clopirac is ananti-inflammatory agent.Dehydroevodiamine is a major bioactive quinazolinealkaloi

19、d isolated from Evodiae Fructus, has anantiarrhythmic effect in guinea-pig ventricularmyocytes.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLIN

20、K https:/www.MedChemE/desoxo-narchinol-a.html Desoxo-narchinol HYPERLINK https:/www.MedChemE/desoxo-narchinol-a.html HYPERLINK https:/www.MedChemE/desoxo-narchinol-a.html A HYPERLINK https:/www.MedChemE/desoxo-narchinol-a.html HYPERLINK https:/www.MedChemE/ethyl-caffeate.html Ethyl HYPERLINK https:/

21、www.MedChemE/ethyl-caffeate.html HYPERLINK https:/www.MedChemE/ethyl-caffeate.html CaffeateCat. No.: HY-N8435 Cat. No.: HY-N6966Desoxo-narchinol A is an orally active and potentanti-inflammatory agent. Desoxo-narchinol A can beisolated from the roots and rhizomes ofNardostachys jatamansi. Desoxo-nar

22、chinol A canbe used for septic shock and inflammatory diseasesresearch.Ethyl Caffeate is a natural phenolic compoundisolated from Bidens pilosa.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg,

23、100 mg HYPERLINK https:/www.MedChemE/furprofen.html Furprofen HYPERLINK https:/www.MedChemE/furprofen.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-1.html HPGDS HYPERLINK https:/www.MedChemE/hpgds-inhibitor-1.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-1.html inhibitor HYPERLINK https:/w

24、ww.MedChemE/hpgds-inhibitor-1.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-1.html 1Cat. No.: HY-106907 Cat. No.: HY-10439Furprofen is an non-steroidal anti-inflammatorydrug (NSAID) with analgesic properties. Furprofenacts via the inhibition of prostaglandin (PGE)synthesis. Furprofen can be tre

25、ated orally for therelief of pain.HPGDS inhibitor 1 is a potent, selective andorally active Hematopoietic Prostaglandin DSynthase (HPGDS) inhibitor with an IC s of 0.650nM and 32 nM in enzyme and cellular assays,respectively. HPGDS inhibitor 1 does not inhibithuman L-PGDS, mPGES, COX-1, COX-2, or 5-

26、LOX.Purity: 99.85%Clinical Data:Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.04%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/hpgds-inhibitor-2.html HPGDS HYPERLINK https:/www.MedChemE/hpgds-inhibitor-2.html HYPERLINK https

27、:/www.MedChemE/hpgds-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/hpgds-inhibitor-2.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-2.html 2 HYPERLINK https:/www.MedChemE/hpgds-inhibitor-2.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-3.html HPGDS HYPERLINK https:/www.MedChemE/hp

28、gds-inhibitor-3.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-3.html inhibitor HYPERLINK https:/www.MedChemE/hpgds-inhibitor-3.html HYPERLINK https:/www.MedChemE/hpgds-inhibitor-3.html 3Cat. No.: HY-126134 Cat. No.: HY-146662HPGDS inhibitor 2 is a highly potent and selectivehematopoietic prosta

29、glandin D synthase(H-PGDS) inhibitor with an IC of 9.9 nM.50HPGDS inhibitor 3 is an orally active and highlypotent peripherally restricted hematopoieticprostaglandin D synthase (H-PGDS) inhibitor withIC50 value of 9.4 nM and EC50 of 42 nM,respectively.Purity: 99.79%Clinical Data: No Development Repo

30、rtedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hPGDS-IN-1.html hPGDS-IN-1 HYPERLINK https:/www.MedChemE/hPGDS-IN-1.html HYPERLINK https:/www.MedChemE/hql-79.html HQL-79Cat. No.: HY-12791 Cat. No.: HY-108

31、259hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12nM in the Fluorescence Polarization Assay or theEIA assay. IC50 value: 12 nM Target: hPGDS Thedetailed information please refer toWO2011044307A1 and WO2010080563A2.Purity: 99.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50

32、 mgHQL-79, a potent, selective and orally activehuman hematopoietic prostaglandin D synthase(H-PGDS) inhibitor, highly selectively inhibitsthe synthesis of PGD , and acts as an2anti-allergic agent, with a K of 0.8 M and andIC of 6 M.50Purity: 99.87%Clinical Data: No Development ReportedSize: 5 mg, 1

33、0 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/isofezolac.html Isofezolac HYPERLINK https:/www.MedChemE/isofezolac.html HYPERLINK https:/www.MedChemE/Limaprost.html Limaprost(LM 22070) Cat. No.: HY-105939 (17,20-dimethyl-2-PGE1; ONO1206; OP1206) Cat. No.: HY-B0683Isofezolac (LM 22070) is a

34、 non-steroidalanti-inflammatory drug (NSAID) that inhibitsprostaglandin-synthetase. Isofezolacanti-inflammatory, and antipyretic properties.Limaprost (OP1206) is a PGE1 analogue and apotent and orally active vasodilator. Limaprostincreases blood flow and inhibits plateletaggregation. Limaprost pain

35、relief, hasantianginal effects, and can be used for ischaemicsymptoms research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.95%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/limaprost-d3.html Limaprost-d3 H

36、YPERLINK https:/www.MedChemE/limaprost-d3.html HYPERLINK https:/www.MedChemE/MF63.html MF63Cat. No.: HY-B0683S Cat. No.: HY-13283Limaprost-d3 (17,20-dimethyl-2-PGE1-d3) is thedeuterium labeled Limaprost. Limaprost (OP1206) isa PGE1 analogue and a potent and orally activevasodilator. Limaprost increa

37、ses blood flow andinhibits platelet aggregation.MF63 is a selective mPGES-1 inhibitor with an IC50of 0.9 nM and 1.3 nM for pig mPGES-1 and humanmPGES-1 enzyme, respectively.Purity: 98%Clinical Data:Size: 500 g, 5 mgPurity: 99.05%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50

38、 mg, 100 mg HYPERLINK https:/www.MedChemE/mpges1-in-3.html mPGES1-IN-3 HYPERLINK https:/www.MedChemE/mpges1-in-3.html HYPERLINK https:/www.MedChemE/pf-4693627.html PF-4693627Cat. No.: HY-100864 Cat. No.: HY-125415mPGES1-IN-3 (Compound 17d) is a potent andselective microsomal prostaglandin E2 synthas

39、e-1(mPGES-1) inhibitor, which exhibits excellentmPGES-1 enzyme (IC : 8 nM), cell (A549 IC : 16.2450 50nM) and human whole blood potency (IC : 249.9 nM).50PF-4693627 is a potent, selective and orallybioavailable microsomal prostaglandin Esynthase-1 (mPGES-1) inhibitor (IC =3 nM) for50the treatment of

40、 inflammation caused byosteoarthritis (OA) and rheumatoid arthritis (RA).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.88%Clinical Data: No Development ReportedSize: 10 mg HYPERLINK https:/www.MedChemE/pf-9184.html PF-9184Cat. No.: HY-19622 HYPERLINK https:/www.MedChemE

41、/2_3H_-Furanone,_3-3,5-bis_1,1-dimethylethyl_-4-hydroxyphenylmethylenedihydro-,_E_-.html PGS-IN-1(KME-4) Cat. No.: HY-101587PF-9184 is a potent and highly selective inhibitorof human microsomal prostaglandin E synthase-1(mPGES-1), with an IC of 16.5 nM. PF-918450inhibits IL-1-induced PGE synthesis i

42、n vitro.2PGS-IN-1 is a potent inhibitor of prostaglandinsynthetase (PGS) with an IC of 0.28 M; also50inhibits 5-lipoxygenase with an IC of 1.05 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.51%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg HYPE

43、RLINK https:/www.MedChemE/Pranoprofen.html Pranoprofen HYPERLINK https:/www.MedChemE/Pranoprofen.html HYPERLINK https:/www.MedChemE/Sinensetin.html SinensetinCat. No.: HY-B0336(Pedalitin permethyl ether) Cat. No.: HY-N0297Pranoprofen is a non-steroidal anti-inflammatoryagent (NSAID) for the research

44、 of keratitis orother ophthalmology diseases. Pranoprofeninhibit COX-1 and COX-2 enzymes, thus blockingarachidonic acid converted to eicosanoids andreducing prostaglandins synthesis.Sinensetin is a methylated flavone found incertain citrus fruits. pocess potentantiangiogenesis and anti-inflammatory,

45、 sinensetinenhances adipogenesis and lipolysis.Purity: 99.37%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 99.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/sinensetin-d3.html Sinensetin-d3 HYPERLINK https:/www.MedChemE/si

46、nensetin-d3.html HYPERLINK https:/www.MedChemE/Suprofen.html SuprofenCat. No.: HY-N0297S(TN-762) Cat. No.: HY-B0270Sinensetin-d3 is the deuterium labeled Sinensetin.Sinensetin is a methylated flavone found incertain citrus fruits. pocess potentantiangiogenesis and anti-inflammatory, sinensetinenhanc

47、es adipogenesis and lipolysis.Suprofen (TN-762) is a non-steroidalanti-inflammatory drug (NSAID).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 99.11%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedC

48、hemE HYPERLINK https:/www.MedChemE/suprofen-d3.html Suprofen-d3 HYPERLINK https:/www.MedChemE/suprofen-d3.html HYPERLINK https:/www.MedChemE/tfc-007.html TFC HYPERLINK https:/www.MedChemE/tfc-007.html HYPERLINK https:/www.MedChemE/tfc-007.html 007Cat. No.: HY-B0270S Cat. No.: HY-110167Suprofen-d3 (T

49、N-762-d3) is the deuterium labeledSuprofen. Suprofen (TN-762) is a non-steroidalanti-inflammatory drug (NSAID).TFC-007, a selective hematopoietic prostaglandin Dsynthase (H-PGDS) inhibitor, show high inhibitoryactivity against H-PGDS enzyme (IC value of 8350nM).Purity: 98%Clinical Data:Size: 2.5 mg,

50、 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ys121.html YS121Cat. No.: HY-111140 HYPERLINK https:/www.MedChemE/zaloglanstat.html Zaloglanstat(ISC-27864; GRC-27864) Cat. No.: HY-139589YS121 is a dual inhibitor of microsomalprostaglandin E2 synthase-1 (mPGES-1; IC =3.450M) and 5-lipoxygenase (5-LOX; IC =6.5 M).50YS121 dose- dependently reduces PGE2 productionwith EC =12 M in IL-1-stimulated A549 cells.50Zaloglan