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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

NOD-like Receptor (NLR)

The nucleotide-binding oligomerization domain-like receptors, or NOD-like receptors (NLRs) (also known as nucleotide-binding leucine-rich repeat receptors), are intracellular sensors of pathogen-associated molecular patterns (PAMPs) that enter the cell via phagocytosis or pores, and damage-associated molecular patterns (DAMPs) that are associated with cell stress. They are types of pattern recognition receptors (PRRs), and play key roles in the regulation of innate immune response. NLRs can cooperate with toll-like receptors (TLRs) and regulate inflammatory and apoptotic response. They are found in lymphocytes, macrophages, dendritic cells and also in non-immune cells, for example in epithelium. NLRs are highly conserved through evolution. Their homologs have been discovered in many different animal species (APAF1) and also in the plant kingdom (disease-resistance R protein).

Filter HomeSignaling PathwaysImmunology/InflammationNOD-like Receptor (NLR)

MCC950 sodium

T6887256373-96-3

MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1.

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NOD-IN-1

T3587132819-92-2

NOD-IN-1 (Compound 4) is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors.

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Nodinitib-1

T6591799264-47-4

Nodinitib-1 (CID-1088438) is a potent and selective NOD1 inhibitor with an IC50 of 0.56 μM.

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Emlenoflast

T92221995067-59-8

Emlenoflast (MCC7840) is a selective inhibitor of NLRP3 inflammasome.

$116

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Troxerutin

T07727085-55-4

Troxerutin (Trihydroxyethylrutin), a natural bioflavonoid, is isolated from Sophora japonica. It has many benefits and medicinal properties.

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CY-09

T41641073612-91-5

CY-09 is an NLRP3 inhibitor.

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Trimethylamine N-oxide

T412451184-78-7

Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.

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Ruscogenin

T6S1256472-11-7

1. Ruscogenin has anti-inflammatory activity, suppressed zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner, 2. Ruscogenin inhibited adhesion of leukocytes to a human umbilical vein endothelial cell line (ECV34) injured by tumor necrosis factor-alpha (TNF-alpha) in a concentration-dependent manner. 3. Ruscogenin significantly attenuate LPS-induced acute lung injury via inhibiting expressions of TF and iNOS and NF-kappa B p65 activation.

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JC2-11

T77579937820-89-8

JC2-11 is an inhibitory compound for inflammation.JC2-11 inhibits the recruitment domain-containing proteins NLRC 4, atypical in melanoma 2 (AIM 2) and atypical (NC) inflammatory vesicles by disrupting reactive oxygen species (ROS) production and caspase-1 activity.JC2-11 reduces caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) activity in inflammatory vesicles. JC2-11 reduced caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) release from inflammatory vesicles.

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YQ128

T133752454246-18-3

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM and exhibits significant anti-inflammatory activity.

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Dapansutrile

T1505254863-37-5

Dapansutrile is a potent, selective and orally active NLRP3 inflammasome inhibitor, with Anti-inflammatory and analgesic activity.

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INF39

T4217866028-26-4

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

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CORM-3

T6454475473-26-8

CORM-3 is a carbon monoxide-releasing molecule with anti-inflammatory and cardioprotective activity.

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Stavudine

T14043056-17-5

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

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NLRP3-IN-2

T323016673-34-0

NLRP3-IN-2 (5-Chloro-N-(p-sulfamoylphenethyl)-o-anisamide), an intermediate capable of synthesizing glibenclamide, exerts an inhibitory effect on the formation of NLRP3 inflammatory vesicles in cardiomyocytes, limiting infarct size after myocardial ischemia reperfusion in mice and has no effect on metabolism.

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Arglabin

TQ016584692-91-1

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

$106

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Usnoflast

T798642455519-86-3

Usnoflast functions as an NLRP3 modulator and also serves as a non-steroidal anti-inflammatory agent (NSAID) [1].

$439

8-10 weeks

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INF200

T79446

INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-induced metaflammation and demonstrates anti-inflammatory effects by reducing IL-1β release in human macrophages at a concentration of 10 μM. Additionally, it enhances glucose and lipid profiles, diminishes systemic inflammation and cardiac dysfunction biomarkers, notably BNP, and ameliorates myocardial damage linked to ischemia/reperfusion injury (IRI) as assessed by hemodynamic parameters [1].

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NLRP3-IN-17

T781682254432-75-0

NLRP3-IN-17 is a potent, selective, and orally active inhibitor of the NLRP3 inflammasome with an IC50 of 7 nM, effectively inhibiting NLRP3-dependent IL-1β secretion in mice, making it valuable for chronic inflammatory disease research [1].

$140

5 days

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NLRP3-IN-21

T788942956791-61-8

NLRP3-IN-21 (compound L38) is an inhibitor of the NLRP3 inflammasome with anti-inflammatory properties, suppressing inflammasome activation and pyroptosis by inhibiting gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly [1].

$1,520

8-10 weeks

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NLRP3-IN-16

T730152906872-59-9

NLRP3-IN-16 is a potent, selective inhibitor of the NLRP3 inflammasome, effectively reducing IL-1β release with an IC50 of 0.065 μM, and is primarily utilized in inflammation research [1].

$1,520

6-8 weeks

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TriDAP

T80267877462-71-0

TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid), a biologically active peptide, functions as a specific Nod1 activator.

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Oxidized low density lipoprotein (Human)

T200276

Oxidized low density lipoprotein (Human) (Human ox-LDL) plays a crucial role in atherogenesis and contributes to endothelial dysfunction through the cytoplasmic adapter protein TRAF3IP2. This compound also promotes endothelial cell activation, leads to increased production of adhesion molecules, and reduces eNOS activity and NO production. Additionally, Human ox-LDL activates the NLRP3 inflammasome in macrophages.

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NLRP3-IN-49

T200567

NLRP3-IN-49 (compound Z48) is a potent and specific inhibitor of NLRP3, displaying IC50 values of 0.26 μM in THP-1 cells and 0.21 μM in mouse bone marrow-derived macrophages. It directly binds to the NLRP3 protein with a dissociation constant (Kd) of 1.05 μM, effectively preventing the assembly and activation of the NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 is utilized in the research of inflammatory bowel disease.

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NOD1-IN-1

T200671687627-78-7

NOD1 2-IN-1 (Compound 2) is a potent inhibitor of RIPK2 with an IC50 value of 0.65 nM as determined by the ADP-Glo assay. It selectively inhibits the NOD1 pathway, with an IC50 of 33 nM, effectively blocking the production of pro-inflammatory cytokines and thereby reducing inflammatory responses. This compound has potential applications in the research of colitis.

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10-14 weeks

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NLRP3-IN-46

T200610

NLRP3-IN-46 (Compound 3k) activates the cholinergic anti-inflammatory pathway involved in neuro-immune modulation, thereby inhibiting the activation of the NLRP3 inflammasome. Furthermore, NLRP3-IN-46 suppresses the production of IL-1β in THP-1 cells induced by Uric acid sodium, making it relevant for research in gouty arthritis.

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Selnoflast potassium

T78614

Selnoflast (potassium) (example 6), is an NLRP3 inhibitor.

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JT002

T788222238820-43-2

JT002 is an orally active NLRP3 inflammasome inhibitor that decreases the production of NLRP3-dependent proinflammatory cytokines (such as IL-1β, IL-1α, IL-18) and pyroptosis, as well as inhibits the formation of the NLRP3 inflammasome complex. Additionally, JT002 mitigates airway hyperresponsiveness and airway neutrophilia in mice [1].

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8-10 weeks

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NLRP3-IN-19

T796952238819-65-1

JT001 (NLRP3-IN-19) is a potent, specific, and orally active NLRP3 inhibitor that impedes the assembly of the NLRP3 inflammasome, suppressing cytokine release and preventing pyroptosis. JT001 is utilized in research on nonalcoholic steatohepatitis and liver fibrosis [1].

$1,520

6-8 weeks

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NLRP3-IN-44

T899533040298-34-5

NLRP3-IN-44 (compound P33), an orally active (approximately 62%) and potent inhibitor of NLRP3, exhibits a dissociation constant (K D) of 17.5 nM. This compound is crucial in the research of diseases mediated by the NLRP3 inflammasome.

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10-14 weeks

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NOD1/2-IN-1

T200582

NOD1 2-IN-1 (Compound 18) is a potent RIPK2 inhibitor, demonstrating an IC50 value of 1.4 nM in the ADP-Glo assay. It blocks the production of pro-inflammatory cytokines by inhibiting the NOD1 NOD2 pathway (IC50 values are 18 nM and 170 nM for NOD1 and NOD2, respectively), thereby reducing inflammatory responses. This compound is utilized in research related to colitis.

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Selnoflast calcium

T786132887416-19-3

Selnoflast calcium (example 6), an NLRP3 inhibitor[1], is a chemical compound designed to suppress the activity of the NLRP3 inflammasome.

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Anti-neuroinflammation agent 1

T79590

Anti-neuroinflammation Agent 1 effectively modulates BV2 microglia cell polarization, shifting from an M1 to an M2 phenotype [1].

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NLRP3-IN-20

T797332428478-22-0

NLRP3-IN-20 (compound 11) is an orally administered inhibitor targeting the NLRP3 inflammasome, exhibiting potent inhibition with an IC50 of 25 nM against IL-1β secretion. It possesses excellent pharmacokinetic properties and has shown significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis [1].

$1,520

6-8 weeks

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D359-0396

T826211031977-31-7

D359-0396, an orally active NLRP3 inflammasome inhibitor, mitigates pyroptosis and reduces IL-1β release in macrophages by inhibiting the oligomerization of NLRP3, ASC, and the cleavage of GSDMD. The compound is effective in alleviating Experimental Autoimmune Encephalomyelitis (EAE) and enhances survival following septic shock in mice [1].

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8-10 weeks

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NLRP3 agonist 2

T81667

NLRP3 agonist 2 (compound 22) is an orally active agent that activates Caspase-1 in THP1 cells [1].

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NLRP3-IN-18

T781802769040-06-2

NLRP3-IN-18, also known as compound 13, is a potent inhibitor of NLRP3, demonstrating an IC50 value of ≤1.0 µM [1].

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8-10 weeks

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iE-DAP

T80268592520-07-5

iE-DAP is a biologically active peptide that functions as a NOD1 agonist.

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NLRP3-IN-23

T81665

NLRP3-IN-23 (Compound 15C) is an inhibitor that significantly impedes heme-mediated activation of the NLRP3 inflammasome at a concentration of 0.1 μM [1].

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CIB-1476

T200261

CIB-1476, a caspase-1 inhibitor, effectively reduces joint swelling in mouse models of arthritis and demonstrates lasting anti-inflammatory effects. This compound achieves its benefits by blocking IL-1β production, NF-κB activation, and GSDMD-mediated pyroptosis, all of which are triggered by the NLRP3 inflammasome.

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JT001 sodium

T79696

JT001 (NLRP3-IN-19) sodium is a potent, specific, and orally active NLRP3 inhibitor that impedes NLRP3 inflammasome assembly, curbing cytokine release and averting pyroptosis. It is utilized in research focused on nonalcoholic steatohepatitis and liver fibrosis [1].

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M-TriDAP

T8027360230-21-9

M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a bioactive peptide that functions as a NOD1 2 agonist.

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NLRP3-IN-22

T816661193329-98-4

NLRP3-IN-22 (Compound II-4) is an NLRP3 inhibitor with a 67% inhibition rate at 10 μM [1].

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8-10 weeks

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RC529-MDP

T200123

RC529-MDP is an immunological adjuvant that couples Toll-like receptors (TLR4a) and NOD-like receptors (NOD2a) to enhance the innate immune response through the TLR4 and NOD2 signaling pathways. In mouse models, RC529-MDP induces high levels of the cytokine interleukin-related factor (IL-6), highlighting its immunostimulatory activity. Additionally, when injected into mice models with ovalbumin (OVA), RC529-MDP elevates OVA-specific antibody responses, T cell responses, and the proportion of memory T cells.

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NLRP3-IN-45

T200214

NLRP3-IN-45 (D6) serves as an inhibitor specifically targeting the NLRP3 inflammasome, demonstrated through its ability to curb the activity of IL-1β (IC 50 = 41.79 nM). It effectively prevents the activation of the NLRP3 inflammasome while sparing the initial stages of its activation process. Furthermore, NLRP3-IN-45 has been shown to selectively inhibit NLRP3 inflammasome activation in the LPS-induced acute lung injury (ALI) mouse model.

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NLRP3-IN-48

T200495

NLRP3-IN-48 is an inhibitor of NLRP3. It suppresses the activation of the NLRP3 inflammasome by targeting the NLRP3 protein, thereby interfering with the assembly of the NLRP3 inflammasome. Additionally, NLRP3-IN-48 exhibits anti-inflammatory activity in a DSS-induced acute colitis model in mice.

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YM-I-26

T2006492585015-90-1

YM-I-26 is a selective inhibitor of the NLRP3 inflammasome. This compound enhances the phagocytic activity of β-amyloid in murine microglial BV2 cells and reduces the production of IL-1β and IL-10. YM-I-26 is useful for research into inflammation-related immunomodulatory activities.

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10-14 weeks

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