NOD-like-Receptor-NLR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html NOD-like HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html Receptor HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK htt

2、ps:/www.MedChemE/Targets/NOD-like Receptor (NLR).html (NLR)Nucleotide oligomerization domain (NOD)-like receptors (NLRs) are critical cytoplasmic pattern-recognition receptors (PRRs) thatplay an important role in the host innate immune response and immunity homeostasis. There are 23 NLR family membe

3、rs inhumans and at least 34 NLR genes in mice. NLRs are expressed in many cell types including immune cells and epithelial cells,although certain NLR family members are expressed primarily in phagocytes including macrophages and neutrophils. The NLRfamily are most commonly classified according to th

4、eir N-terminal domain, falling into one of four subfamilies; NLRA, NLRB, NLRCand NLRP.The NLRs recognize various ligands from microbial pathogens (peptidoglycan, flagellin, viral RNA, fungal hyphae, etc.), host cells(ATPs, cholesterol crystals, uric acid, etc.), and environmental sources (alum, asbe

5、stos, silica, alloy particles, UV radiation, skinirritants, etc.). Most NLRs act as PRRs, recognizing the above ligands and activate inflammatory responses. However, some NLRsmay not act as PRRs but instead respond to cytokines such as interferons. The activated NLRs show various functions that can

6、bedivided into four broad categories: inflammasome formation, signaling transduction, transcription activation, and autophagy.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html NOD-like HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:

7、/www.MedChemE/Targets/NOD-like Receptor (NLR).html Receptor HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html (NLR) HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Tar

8、gets/NOD-like Receptor (NLR).html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html Agonists, HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-l

9、ike Receptor (NLR).html Antagonists, HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html Activators HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Rece

10、ptor (NLR).html & HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html HYPERLINK https:/www.MedChemE/Targets/NOD-like Receptor (NLR).html Modulators HYPERLINK https:/www.MedChemE/racemic-11-12-eet.html ()11(12)-EET(11,12-EET) Cat. No.: HY-130494 HYPERLINK https:/www.MedChemE/racemic-11

11、-12-eet-d11.html ()11(12)-EET-d11()11,12-EET-d11) Cat. No.: HY-130494S()11(12)-EET is a NLRP3 inflammasome inhibitor.()11(12)-EET can be used for the research ofanti-inflammatory, angiogenic andcardioprotective.()11(12)-EET-d11 ()11,12-EET-d11) is thedeuterium labeled ()11(12)-EET. ()11(12)-EET isa

12、NLRP3 inflammasome inhibitor. ()11(12)-EET canbe used for the research of anti-inflammatory,angiogenic and cardioprotective.Purity: 98%Clinical Data: No Development ReportedSize: 25 g, 50 gPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Arglabin.html A

13、rglabin(+)-Arglabin) Cat. No.: HY-16059 HYPERLINK https:/www.MedChemE/bms-986299.html BMS-986299Cat. No.: HY-139396Arglabin (+)-Arglabin), a natural productisolated from Artemisia glabella, is a NLRP3inflammasome inhibitor. Arglabin showsanti-inflammatory and antitumor activities.BMS-986299 (compoun

14、d 112) is a first-in-classNLRP3 inflammasome agonist with an EC of 1.2850M. (patent WO2018152396A1).Purity: 99.49%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.95%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPER

15、LINK https:/www.MedChemE/cardamonin-1.html Cardamonin(Cardamomin; Alpinetin chalcone) Cat. No.: HY-N0279 HYPERLINK https:/www.MedChemE/corm-3.html CORM-3Cat. No.: HY-100581Cardamonin (Cardamomin) acts as an aryl hydrocarbonreceptor (AhR) activator. Cardamonin alleviatesinflammatory bowel disease by

16、the inhibition ofNLRP3 inflammasome activation via anAhR/Nrf2/NQO1 pathway.CORM-3, a carbon monoxide-releasing molecule,attenuates NF-B p65 nuclear translocation,reduces ROS generation and enhances intracellularglutathione and superoxide dismutase levels.CORM-3 reduces NLRP3 inflammasome activation.

17、Purity: 98.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cp-424174.html CP-424174 HYPERLINK https:/www.MedChemE/cp-424174.html HYPERLINK https:/www.MedChemE/CY-0

18、9.html CY-09Cat. No.: HY-119721 Cat. No.: HY-103666CP-424174 is a reversible inhibitor against IL-1processing with an IC of 210 nM.CP-42417450indirectly inhibits NLRP3.CY-09 is a selective and direct NLRP3 inhibitor.CY-09 directly binds to the ATP-binding motif ofNLRP3 NACHT domain and inhibits NLRP

19、3 ATPaseactivity, resulting in the suppression of NLRP3inflammasome assembly and activation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Dapansutril

20、e.html Dapansutrile HYPERLINK https:/www.MedChemE/Dapansutrile.html HYPERLINK https:/www.MedChemE/mcc7840.html EmlenoflastCat. No.: HY-17629(MCC7840) Cat. No.: HY-137245Dapansutrile is a potent, selective and orallyactive inhibitor of NLRP3 inflammasome.Anti-inflammatory, analgesic activity.Emlenofl

21、ast (MCC7840), a sulfonylurea, is a potentand selective inhibitor of NLRP3 inflammasome,with an IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/mcc7840-sodium.html Emlenoflast HYPERLINK https:/www

22、.MedChemE/mcc7840-sodium.html HYPERLINK https:/www.MedChemE/mcc7840-sodium.html sodium(MCC7840 sodium) Cat. No.: HY-137245A HYPERLINK https:/www.MedChemE/gsk717.html GSK717Cat. No.: HY-136555Emlenoflast (MCC7840) sodium, a sulfonylurea, is apotent and selective inhibitor of NLRP3inflammasome, with a

23、n IC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/jc-171.html JC-171 HYPERLINK https:/www.MedChemE/jc-171.html HYPERLINK https:/www.MedChemE/jc124.html JC124Cat. No.: HY-117432 Cat. No.: HY-120007JC-171 is a selective NLRP3 inflammasomeinhibitor, with an

24、 IC of 8.45 M for inhibiting50LPS/ATP-induced interleukin-1 (IL-1) releasefrom J774A.1 macrophages.JC124 is a specific NLRP3 inflammasome inhibitor.JC124 has anti-inflammatory and neuroprotectiveeffects.Purity: 99.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgP

25、urity: 97.13%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/licochalcone-b.html Licochalcone HYPERLINK https:/www.MedChemE/licochalcone-b.html HYPERLINK https:/www.MedChemE/licochalcone-b.html B HYPERLINK https:/www.MedChemE/licochalcone-b.html H

26、YPERLINK https:/www.MedChemE/MCC950.html MCC950Cat. No.: HY-N0373(CP-456773; CRID3) Cat. No.: HY-12815Licochalcone B is an extract from the root ofGlycyrrhiza inflate.MCC950 (CP-456773; CRID3) is a potent andselective NLRP3 inhibitor with IC s of 7.5 and508.1 nM in BMDMs and HMDMs, respectively.Puri

27、ty: 99.93%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/MCC950-sodium.html MCC950 HYPERLINK https:/www.MedChemE/MCC950-sodium.html HYPERLINK https

28、:/www.MedChemE/MCC950-sodium.html sodium HYPERLINK https:/www.MedChemE/MCC950-sodium.html HYPERLINK https:/www.MedChemE/muramyl-dipeptide.html Muramyl HYPERLINK https:/www.MedChemE/muramyl-dipeptide.html HYPERLINK https:/www.MedChemE/muramyl-dipeptide.html dipeptide(CP-456773 sodium; CRID3 sodium sa

29、lt) Cat. No.: HY-12815A (MDP) Cat. No.: HY-127090MCC950 sodium (CP-456773 sodium; CRID3 sodiumsalt) is a potent, selective NLRP3 inhibitor withIC s of 7.5 and 8.1 nM in BMDMs and HMDMs,50respectively.Muramyl dipeptide (MDP) is a syntheticimmunoreactive peptide, consisting of N-acetylmuramic acid att

30、ached to a short amino acid chainof L-Ala-D-isoGln. Muramyl dipeptide is an inducerof bone formation through induction of Runx2.Purity: 99.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: Phase 4Size: 1 mg, 5 mg, 10 mg, 25 mgwww.

31、MedChemE 3 HYPERLINK https:/www.MedChemE/muscone.html Muscone HYPERLINK https:/www.MedChemE/muscone.html HYPERLINK https:/www.MedChemE/nigericin.html NigericinCat. No.: HY-N0633 Cat. No.: HY-127019Muscone is the main active monomer of traditionalChinese medicine musk. Muscone inhibits NF-B andNLRP3

32、inflammasome activation. Muscone remarkablydecreases the levels of inflammatory cytokines(IL-1, TNF- and IL-6), and ultimately improvescardiac function and survival rate.Nigericin is an antibiotic derived fromStreptomyces hygroscopicus that act as aK+/H+ ionophore, promoting K+/H+ exchangeacross mit

33、ochondrial membranes.Nigericin can be aNLRP3 activator that induces the release ofIL-1 as a NALP3-dependent manner.Purity: 98.0%Clinical Data: No Development ReportedSize: 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Nigericin-so

34、dium-salt.html Nigericin HYPERLINK https:/www.MedChemE/Nigericin-sodium-salt.html HYPERLINK https:/www.MedChemE/Nigericin-sodium-salt.html sodium HYPERLINK https:/www.MedChemE/Nigericin-sodium-salt.html HYPERLINK https:/www.MedChemE/Nigericin-sodium-salt.html salt HYPERLINK https:/www.MedChemE/Niger

35、icin-sodium-salt.html HYPERLINK https:/www.MedChemE/nlrp3-antagonist-1.html NLRP3 HYPERLINK https:/www.MedChemE/nlrp3-antagonist-1.html HYPERLINK https:/www.MedChemE/nlrp3-antagonist-1.html antagonist HYPERLINK https:/www.MedChemE/nlrp3-antagonist-1.html HYPERLINK https:/www.MedChemE/nlrp3-antagonis

36、t-1.html 1Cat. No.: HY-100381 Cat. No.: HY-143563Nigericin sodium salt is an antibiotic fromStreptomyces hygroscopicus that works by actingas an H+, K+, and Pb2+ ionophore, a NLRP3activator.NLRP3 antagonist 1 is a potent antagonist ofNLRP3. NLRP3 is mainly expressed in macrophagesand neutrophils and

37、 is involved in the bodysintrinsic immunity against pathogenic infectionsand stress injury.Purity: 95.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nlrp3-modulators-1.html NLRP3 HYPERLINK https

38、:/www.MedChemE/nlrp3-modulators-1.html HYPERLINK https:/www.MedChemE/nlrp3-modulators-1.html modulators HYPERLINK https:/www.MedChemE/nlrp3-modulators-1.html HYPERLINK https:/www.MedChemE/nlrp3-modulators-1.html 1 HYPERLINK https:/www.MedChemE/nlrp3-modulators-1.html HYPERLINK https:/www.MedChemE/nl

39、rp3-in-2.html NLRP3-IN-2Cat. No.: HY-103715 Cat. No.: HY-W011082NLRP3 modulators 1 is the potent modulator ofNLRP3.NLRP3-IN-2, an intermediate substrate in thesynthesis of glyburide, inhibits the formation ofthe NLRP3 inflammasome in cardiomyocytes andlimits the infarct size following myocardialisch

40、emia/reperfusion in the mouse, withoutaffecting glucose metabolism.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.52%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nlrp3-in-4.html NLRP3-IN-4 HYPERLINK https:/www.MedChe

41、mE/nlrp3-in-4.html HYPERLINK https:/www.MedChemE/nlrp3-in-5.html NLRP3-IN-5Cat. No.: HY-132892 Cat. No.: HY-145087NLRP3-IN-4 is potent and orally active NLRP3inflammasome inhibitor with inflammatory activityfor colitis.NLRP3-IN-5 is a NLRP3 inflammasome inhibitor(WO2016131098 (N-(4-chloro-2,6-dimeth

42、ylphenyl)carbamoyl)-4-(2-hydroxypropan-2-l)furan-2-sulfonamide).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/nlrp3-in-8.html NLRP3-IN-8 HYPERLINK https:/www.MedChemE/nlrp3-in-8.html HY

43、PERLINK https:/www.MedChemE/nlrp3-in-nbc6.html NLRP3-IN-NBC6Cat. No.: HY-146594 Cat. No.: HY-131040NLRP3-IN-8 (compound 27) is an orally active,directly binding NLRP3 inflammasome inhibitorwith an IC value of 1.23 M against IL-1 .50NLRP3-IN-8 has good metabolic stability to livermicrosomes (t = 138.

44、63 min), and has almost no1/2toxicity (against L02: IC 100 M).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgNLRP3-IN-NBC6 is a potent, selective NLRP3inflammasome inhibitor (IC = 574 nM) that acts50independently of Ca2+.Purity: 99.0%Clinical Data: No Development ReportedSize: 5

45、mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/NOD-IN-1.html NOD-IN-1 HYPERLINK https:/www.MedChemE/NOD-IN-1.html HYPERLINK https:/www.MedChemE/nod1-2-antagonist-1.html NOD1/2 HYPERLINK https:/www.MedChemE/nod1-2-antagonist-1.html HYPERLINK https:/www.MedC

46、hemE/nod1-2-antagonist-1.html antagonist-1Cat. No.: HY-100691 Cat. No.: HY-146034NOD-IN-1 is a potent mixed inhibitor ofnucleotide-binding oligomerization domain(NOD)-like receptors, NOD1 and NOD2, with IC of505.74 M and 6.45 M, respectively.Purity: 99.70%Clinical Data: No Development ReportedSize:

47、10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgNOD1/2 antagonist-1 (compound 36b) is a potentNOD1/2 (nucleotide-binding oligomerizationdomain-like receptor 1/2) dual antagonist, withIC50 values of 1.13 (NOD1) and 0.77 M (NOD2),respectively. NOD1/2 antagonist-1 has a acceptableT (67.6 min).1/2Purity: 98

48、%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Nodinitib-1.html Nodinitib-1(ML130; CID-1088438) Cat. No.: HY-18639 HYPERLINK https:/www.MedChemE/qs-21.html QS-21(Stimulon) Cat. No.: HY-101092Nodinitib-1 (ML130;CID-1088438) is a NOD1inhibitor with an IC of 0.56

49、M.50QS-21, an immunostimulatory saponin, could be usedas a potent vaccine adjuvant. QS-21 stimulatesTh2 humoral and Th1 cell-mediated immuneresponses through action on antigen presentingcells (APCs) and T cells.Purity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg,

50、 50 mg, 100 mgPurity: 97.64%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ruscogenin.html Ruscogenin HYPERLINK https:/www.MedChemE/ruscogenin.html HYPERLINK https:/www.MedChemE/selnoflast.html SelnoflastCat. No.: HY-N0496 Cat. No.: HY-132831Ruscogenin, an impo

51、rtant steroid sapogenin derivedfrom Ophiopogon japonicus, attenuates cerebralischemia-induced blood-brain barrier dysfunctionby suppressing TXNIP/NLRP3 inflammasome activationand the MAPK pathway and exerts significantanti-inflammatory and anti-thrombotic activities.Selnoflast (example 6) is a NLRP3

52、 inhibitor(extracted from patent WO2019008025).Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 98.21%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/soyasaponin-ii.html Soyasaponin HYPERLINK https:/www.MedCh

53、emE/soyasaponin-ii.html HYPERLINK https:/www.MedChemE/soyasaponin-ii.html II HYPERLINK https:/www.MedChemE/soyasaponin-ii.html HYPERLINK https:/www.MedChemE/stavudine.html StavudineCat. No.: HY-122920(d4T) Cat. No.: HY-B0116Soyasaponin II is a saponin with antiviralactivity. Soyasaponin II inhibits

54、the replicationof HSV-1, HCMV, influenza virus, and HIV-1.Soyasaponin II shows potent inhibition on HSV-1replication.Stavudine (d4T) is an orally active nucleosidereverse transcriptase inhibitor (NRTI). Stavudinehas activity against HIV-1 and HIV-2. Stavudine alsoinhibits the replication of mitochon

55、drial DNA(mtDNA).Purity: 99.81%Clinical Data: No Development ReportedSize: 1 mgPurity: 99.67%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/stavudine-sodium.html Stavudine HYPERLINK https:/www.MedChemE/stavudine-sodium.html HYPERLINK https:/www.MedChemE/stavudi

56、ne-sodium.html sodium HYPERLINK https:/www.MedChemE/stavudine-sodium.html HYPERLINK https:/www.MedChemE/stavudine-d4.html Stavudine-d4(d4T sodium) Cat. No.: HY-B0116ACat. No.: HY-B0116SStavudine (d4T) sodium is an orally activenucleoside reverse transcriptase inhibitor (NRTI).Stavudine sodium has ac

57、tivity against HIV-1 andHIV-2. Stavudine sodium also inhibits thereplication of mitochondrial DNA (mtDNA).Stavudine-d4 is the deuterium labeled Stavudine.Stavudine (d4T) is an orally active nucleosidereverse transcriptase inhibitor (NRTI). Stavudinehas activity against HIV-1 and HIV-2. Stavudine als

58、oinhibits the replication of mitochondrial DNA(mtDNA).Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/trimethylamine-n-oxide.html Trimethylamine HYPERLINK https:/www.MedChemE/trimethylamine-n-oxide.html HYPERLINK https:/www.MedChemE/trimethylamine-n-oxide.html N-oxide HYPERLINK https:/www.MedChemE/trimethylamine-n-oxide.html HYPERLINK https:/www.MedChemE/trimethylamine-d9-n-ox