TNF-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html TNF HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html ReceptorTumor Necrosis Factor Receptor; TNFRTumor necrosis factor (TNF) is a major mediator of apoptosis as well as inflammation and imm

2、unity, and it has been implicated inthe pathogenesis of a wide spectrum of human diseases, including sepsis, diabetes, cancer, osteoporosis, multiple sclerosis,rheumatoid arthritis, and inflammatory bowel diseases.TNF- is a 17-kDa protein consisting of 157 amino acids that is a homotrimer in solutio

3、n. In humans, the gene is mapped tochromosome 6. Its bioactivity is mainly regulated by soluble TNF-binding receptors. TNF- is mainly produced by activatedmacrophages, T lymphocytes, and natural killer cells. Lower expression is known for a variety of other cells, including fibroblasts,smooth muscle

4、 cells, and tumor cells. In cells, TNF- is synthesized as pro-TNF (26 kDa), which is membrane-bound and is releasedupon cleavage of its pro domain by TNF-converting enzyme (TACE).Many of the TNF-induced cellular responses are mediated by either one of the two TNF receptors, TNF-R1 and TNF-R2, both o

5、fwhich belong to the TNF receptor super-family. In response to TNF treatment, the transcription factor NF-B and MAP kinases,including ERK, p38 and JNK, are activated in most types of cells and, in some cases, apoptosis or necrosis could also be induced.However, induction of apoptosis or necrosis is

6、mainly achieved through TNFR1, which is also known as a death receptor. Activationof the NF-B and MAPKs plays an important role in the induction of many cytokines and immune-regulatory proteins and is pivotalfor many inflammatory responses.www.MedChemE 12 Tel: 609-228-6898 Fax: 609-228-5909 Email: s

7、alesMedChemE HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html TNF HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html Receptor HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html Inhibitor

8、s, HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html Agonists, HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK

9、 https:/www.MedChemE/Targets/TNF-alpha.html Activators HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html & HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html HYPERLINK https:/www.MedChemE/Targets/TNF-alpha.html Inducers HYPERLINK https:/www.M

10、edChemE/rac-benpyrine.html (Rac)-Benpyrine HYPERLINK https:/www.MedChemE/rac-benpyrine.html HYPERLINK https:/www.MedChemE/rac-bio8898.html (Rac)-BIO8898Cat. No.: HY-133807A Cat. No.: HY-122663(Rac)-Benpyrine, a racemate of Benpyrine, is apotent and orally active TNF- inhibitor.(Rac)-Benpyrine has th

11、e potential for TNF-mediated inflammatory and autoimmune diseaseresearch.(Rac)-BIO8898 is a CD40-CD154 co-stimulatoryinteraction inhibitor. (Rac)-BIO8898 inhibits CD154binding to CD40-Ig with an IC of 25 M.50Purity: 99.30%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 10

12、0 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/1-4-dicaffeoylquinic-acid.html 1,4-Dicaffeoylquinic HYPERLINK https:/www.MedChemE/1-4-dicaffeoylquinic-acid.html HYPERLINK https:/www.MedChemE/1-4-dicaffeoylquinic-acid.html acid(1,4-DCQA) Cat. No.: H

13、Y-N0358 HYPERLINK https:/www.MedChemE/5-7-dimethoxyflavanone.html 5,7-DimethoxyflavanoneCat. No.: HY-N50541,4-Dicaffeoylquinic acid (1,4-DCQA) is aphenylpropanoid from Xanthii fructus, inhibitsLPS-stimulated TNF- production.5,7-Dimethoxyflavanone shows potent antimutagenicactivity against MeIQ mutag

14、enesis in Ames testusing the S. typhimurium TA100 and TA98 strains.And 5,7-Dimethoxyflavanone significantly anddose-dependently inhibits the inflammatory mediato.Purity: 99.80%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg H

15、YPERLINK https:/www.MedChemE/7-3-4-tri-o-methylluteolin.html 7,3,4-Tri-O-methylluteolin(5-Hydroxy-3,4,7-trimethoxyflavone) Cat. No.: HY-N7012 HYPERLINK https:/www.MedChemE/Adalimumab.html Adalimumab(Anti-Human TNF-alpha, Human Antibody) Cat. No.: HY-P99087,3,4-Tri-O-methylluteolin(5-Hydroxy-3,4,7-tr

16、imethoxyflavone), a flavonoidcompound, possesses potent anti-inflammatoryeffects in LPS-induced macrophage cell linemediated by inhibition of release of inflammatorymediators, NO, PGE2, andAdalimumab is a human monoclonal IgG1 antibodytargeting tumour necrosis factor (TNF-).Purity: 99.28%Clinical Da

17、ta: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 99.62%Clinical Data: LaunchedSize: 1 mg, 5 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-16.html Anti-inflammatory HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-16.html HYPERLINK https:/www.MedChemE/anti-infla

18、mmatory-agent-16.html agent HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-16.html HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-16.html 16 HYPERLINK https:/www.MedChemE/anti-inflammatory-agent-16.html HYPERLINK https:/www.MedChemE/apratastat.html ApratastatCat. No.: HY-143410 Cat. No

19、.: HY-119307Anti-inflammatory agent 16 (compound 14), apeptidomimetic, shows potent anti-inflammatoryactivity. Anti-inflammatory agent 16 reduces TNF,NO, CD40 and CD86 expression level.Apratastat is an orally active, potent, andreversible dual inhibitor of tumor necrosisfactor- converting enzyme (TA

20、CE) and matrixmetalloproteinases (MMPs) .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.28%Clinical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Apremilast.html Apremilast HYPERLINK https:/www.MedChemE/Apremilast.html HYPERLINK https:/www.MedChemE/apremilast-d5.ht

21、ml Apremilast-d5(CC-10004) Cat. No.: HY-12085 (CC-10004-d5) Cat. No.: HY-12085SApremilast (CC-10004) is an orally availableinhibitor of type-4 cyclic nucleotidephosphodiesterase (PDE-4) with an IC of 74 nM.50Apremilast inhibits TNF- release bylipopolysaccharide (LPS) with an IC of 104 nM.50Purity: 9

22、9.87%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgApremilast D5 (CC-10004 D5) is a deuterium labeledApremilast. Apremilast is an orally availableinhibitor of type-4 cyclic nucleotidephosphodiesterase (PDE-4) with an IC of 74 nM.50Apremilast inhibits TNF- release bylipopo

23、lysaccharide (LPS) with an IC of 104 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/aqx-016a.html AQX-016A HYPERLINK https:/www.MedChemE/aqx-016a.html HYPERLINK https:/www.MedChemE/Astilbin.html AstilbinCat. No.: HY-115620 Cat. No.: HY-N0

24、509AQX-016A is an orally active and potent SHIP1agonist. AQX-016A can activate recombinant SHIP1enzyme in vitro and stimulate SHIP1 activity.AQX-016A also can inhibit the PI3K pathway and TNFaproduction, can be useful for various inflammatorydiseases research.Astilbin is a flavonoid compound and enh

25、ancesNRF2 activation. Astilbin also suppresses TNF-expression and NF-B activation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AX-024.html AX-024 HYPERL

26、INK https:/www.MedChemE/AX-024.html HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html AX-024 HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html hydrochlorideCat. No.: HY-107390 Cat. No.: HY-107390AAX-024 is an orally available, first

27、-in-classinhibitor of the TCR-Nck interaction thatselectively inhibits TCR-triggered T cellactivation with an IC 1 nM. AX-024 modulates50cell signaling by targeting SH3 domains.AX-024 hydrochloride is an orally available,first-in-class inhibitor of the TCR-Nckinteraction that selectively inhibitsTCR

28、-triggered T cell activation with an IC 150nM. AX-024 hydrochloride modulates cell signalingby targeting SH3 domains.Purity: 98.0%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.12%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK

29、 https:/www.MedChemE/belantamab.html Belantamab(GSK2857914) Cat. No.: HY-P9980 HYPERLINK https:/www.MedChemE/belimumab.html Belimumab(LymphoStat B) Cat. No.: HY-P9952Belantamab (GSK2857914) is a humanised IgG1anti-BCMA (TNFRSF17) monoclonal antibody.Belantamab can be used in the synthesis ofantibody

30、-drug conjugate (ADC), Belantamabmafodotin.Belimumab (LymphoStat B) is a human IgG1monoclonal antibody that inhibits B-cell activatingfactor (BAFF). Belimumab can be used for systemiclupus erythematosus (SLE) research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinic

31、al Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/benpyrine.html Benpyrine HYPERLINK https:/www.MedChemE/benpyrine.html HYPERLINK https:/www.MedChemE/Bioymifi.html BioymifiCat. No.: HY-133807(DR5 Activator) Cat. No.: HY-18377Benpyrine is a highly specific and orally activeTNF- inhibito

32、r with a K value of 82.1 M.DBenpyrine tightly binds to TNF- and blocks itsinteraction with TNFR1, with an IC value of500.109 M.Bioymifi (DR5 Activator), a potent TRAIL receptorDR5 activator, binds to the extracellular domain(ECD) of DR5 with a K of 1.2 M. Bioymifi candact as a single agent to induce

33、 DR5 clustering andaggregation, leading to apoptosis.Purity: 99.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/C-87.html C

34、 HYPERLINK https:/www.MedChemE/C-87.html HYPERLINK https:/www.MedChemE/C-87.html 87 HYPERLINK https:/www.MedChemE/C-87.html HYPERLINK https:/www.MedChemE/c25-140.html C25-140Cat. No.: HY-100735 Cat. No.: HY-120934C 87 is a novel small-molecule TNF inhibitor;potently inhibits TNF-induced cytotoxicity

35、 withan IC of 8.73 M.50C25-140, a first-in-class, orally active, andfairly selective TRAF6-Ubc13 inhibitor, directlybinds to TRAF6, and blocks the interaction ofTRAF6 with Ubc13. C25-140 lowers TRAF6 activity,reduces NF-B activation, and combatsautoimmunity.Purity: 98.07%Clinical Data: No Developmen

36、t ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.84%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/CDC801.html CDC801Cat. No.: HY-U00179 HYPERLINK https:

37、/www.MedChemE/cis-mulberroside-a.html cis-Mulberroside HYPERLINK https:/www.MedChemE/cis-mulberroside-a.html HYPERLINK https:/www.MedChemE/cis-mulberroside-a.html A(Mulberroside D) Cat. No.: HY-N0619ACDC801 is a potent and orally activephosphodiesterase 4 (PDE4) and tumor necrosisfactor- (TNF-) inhi

38、bitor with IC of 1.1 M50and 2.5 M, respectively.cis-Mulberroside A (Mulberroside D) is thecis-isomer of Mulberroside A. Mulberroside A isone of the main bioactive constituent in mulberry(Morus alba L.).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Deve

39、lopment ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/cleomiscosin-a.html Cleomiscosin HYPERLINK https:/www.MedChemE/cleomiscosin-a.html HYPERLINK https:/www.MedChemE/cleomiscosin-a.html A HYPERLINK https:/www.MedChemE/cleomiscosin-a.html HYPERLINK https:/www.MedChemE/cleomiscosin-a

40、-d3.html Cleomiscosin HYPERLINK https:/www.MedChemE/cleomiscosin-a-d3.html HYPERLINK https:/www.MedChemE/cleomiscosin-a-d3.html A-d3Cat. No.: HY-N3595 Cat. No.: HY-N3595SCleomiscosin A is a coumarino-lignoid from branchof Macaranga adenantha. Cleomiscosin A is activeagainst TNF-alpha secretion of th

41、e mouse peritonealmacrophages.Cleomiscosin A-d3 is the deuterium labeledCleomiscosin A. Cleomiscosin A is acoumarino-lignoid from branch of Macarangaadenantha. Cleomiscosin A is active againstTNF-alpha secretion of the mouse peritonealmacrophages.Purity: 98%Clinical Data: No Development ReportedSize

42、: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cpi-1189.html CPI-1189 HYPERLINK https:/www.MedChemE/cpi-1189.html HYPERLINK https:/www.MedChemE/Cynaropicrin.html CynaropicrinCat. No.: HY-100376 Cat. No.: HY-N2350CPI-1189 is a TNF-

43、release inhibitor withantioxidant and neuroprotective properties.CPI-1189 is used for researches of HIV-associatedneurotoxicity and thus is a candidate forneuroprotective therapy in humans suffered fromHIV-associated CNS disease.Cynaropicrin is a sesquiterpene lactone which caninhibit tumor necrosis

44、 factor (TNF-) releasewith IC s of 8.24 and 3.18 M for murine and50human macrophage cells, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 97.40%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedCh

45、emE/d-trimannuronic-acid.html D-Trimannuronic HYPERLINK https:/www.MedChemE/d-trimannuronic-acid.html HYPERLINK https:/www.MedChemE/d-trimannuronic-acid.html acid HYPERLINK https:/www.MedChemE/d-trimannuronic-acid.html HYPERLINK https:/www.MedChemE/dacetuzumab.html DacetuzumabCat. No.: HY-N7699A Cat

46、. No.: HY-P99015D-Trimannuronic acid, an alginate oligomer isextracted from seaweed. D-Trimannuronic acid caninduce TNF secretion by mouse macrophage celllines. D-Trimannuronic acid can be used for theresearch of pain and vascular dementia.Dacetuzumab (SGN-40) is a humanized IgG1, anti-CD40monoclona

47、l antibody with anti-lymphoma activity.Dacetuzumab kills tumor cells via immune effectorfunctions (antibody-dependent cellularcytotoxicity and phagocytosis ADCC/ADCP).Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLIN

48、K https:/www.MedChemE/DCVC.html DCVC HYPERLINK https:/www.MedChemE/DCVC.html HYPERLINK 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(S-(1E)-1,2-dichloroethenyl-L-cysteine) Cat

49、. No.: HY-19717Cat. No.: HY-N8435DCVC (S-(1E)-1,2-dichloroethenyl-L-cysteine) isa bioactive metabolite of trichloroethylene (TCE).DCVC inhibits pathogen-stimulated pro-inflammatorycytokines IL-1, IL-8, and TNF- release fromtissue cultures.Desoxo-narchinol A is an orally active and potentanti-inflamm

50、atory agent. Desoxo-narchinol A can beisolated from the roots and rhizomes ofNardostachys jatamansi. Desoxo-narchinol A canbe used for septic shock and inflammatory diseasesresearch.Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Da

51、ta: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/dexanabinol.html Dexanabinol(HU-211) Cat. No.: HY-106387 HYPERLINK https:/www.MedChemE/dri-c21045.html DRI-C21045Cat. No.: HY-120323Dexanabinol (HU-211) is an artificiallysynthesized cannabinoid derivative and la

52、ckscannabimimetic effects.DRI-C21045 (compound 10) is a potent and selectiveinhibitor of the CD40-CD40L costimulatoryprotein-protein interaction (PPI) with an IC of500.17 M.Purity: 98.60%Clinical Data: Phase 3Size: 10 mM 1 mL, 1 mgPurity: 98.26%Clinical Data: No Development ReportedSize: 10 mg, 50 m

53、g, 100 mg HYPERLINK https:/www.MedChemE/episappanol.html Episappanol HYPERLINK https:/www.MedChemE/episappanol.html HYPERLINK https:/www.MedChemE/Etanercept.html EtanerceptCat. No.: HY-N9315 Cat. No.: HY-108847Episappanol is a natural compound isolated fromCaesalpinia sappan heartwood with anti-infl

54、ammatoryactivity. Episappanol significantly inhibits theIL-6 and TNF- secretion.Etanercept, a dimeric fusion protein that bindsTNF, acts as a TNF inhibitor. Etanerceptcompetitively inhibits the binding of both TNF-and TNF- to cell surface TNF receptors, renderingTNF biologically inactive.Purity: 98%

55、Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 96.0%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Fisetin.html Fisetin HYPERLINK https:/www.MedChemE/Fisetin.html HYPERLINK https:/www.MedChemE/Forsythoside_B.html Forsythoside HYPERLINK https:/www.MedChem

56、E/Forsythoside_B.html HYPERLINK https:/www.MedChemE/Forsythoside_B.html BCat. No.: HY-N0182 Cat. No.: HY-N0029Fisetin is a natural flavonol found in many fruitsand vegetables with various benefits, such asantioxidant, anticancer, neuroprotection effects.Forsythoside B is a phenylethanoid glycosideis

57、olated from the leaves of Lamiophlomis rotataKudo, a Chinese folk medicinal plant for treatinginflammatory diseases and promoting bloodcirculation. Forsythoside B could inhibitTNF-alpha, IL-6, IB and modulate NF-B.Purity: 98.87%Clinical Data: Phase 2Size: 10 mM 1 mL, 100 mg, 500 mg, 1 gPurity: 99.99

58、%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gamma-glutamylcysteine-tfa.html Gamma-glutamylcysteine HYPERLINK https:/www.MedChemE/gamma-glutamylcysteine-tfa.html HYPERLINK https:/www.MedChemE/gamma-glutamylcysteine-tfa.html

59、TFA HYPERLINK https:/www.MedChemE/gamma-glutamylcysteine-tfa.html HYPERLINK https:/www.MedChemE/Geraniin.html Geraniin(-Glutamylcysteine TFA) Cat. No.: HY-113402ACat. No.: HY-N0472Gamma-glutamylcysteine (-Glutamylcysteine) TFA,an intermediate in glutathione (GSH) synthesis, isa dipeptide served as a

60、n essential cofactor forthe antioxidant enzyme glutathione peroxidase(GPx).Geraniin is a TNF- releasing inhibitor withnumerous activities including anticancer,anti-inflammatory, and anti-hyperglycemicactivities, with an IC of 43 M.50Purity: 98%Clinical Data: No Development ReportedSize: 50 mg, 100 m