Toll-like Receptor (TLR) Antagonist

Toll-like Receptor (TLR) Antagonists (19):

Cat. No.	Product Name	Effect	Purity

HY-139567

Afimetoran	Antagonist	99.37%
Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus).

HY-116961

TH1020	Antagonist	99.60%
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC₅₀ of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.

HY-150751

ODN TTAGGG	Antagonist	99.87%
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.

HY-N0795

Procyanidin B1	Antagonist	99.28%
Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.

HY-150738

ODN 2088	Antagonist
ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.

HY-150738C

ODN 2088 sodium	Antagonist
ODN 2088 sodium is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 sodium shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.

HY-131952

TLR7/8/9-IN-1	Antagonist	98.51%
TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC₅₀ = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).

HY-150751C

ODN TTAGGG sodium	Antagonist	99.87%
ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.

HY-144619

TLR7/8 antagonist 2	Antagonist	99.68%
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC₅₀s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.

HY-120538

CPG-52364	Antagonist	98.49%
CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC₅₀ value of 4.6 nM.

HY-123789

T5342126	Antagonist
T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC₅₀=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC₅₀s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.

HY-N0201R

Atractylenolide I (Standard)	Antagonist
Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

HY-153460

TLR7/8/9 antagonist 2	Antagonist
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC₅₀ values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

HY-150751B

FITC-labeled ODN TTAGGG sodium	Antagonist
FITC-labeled ODN TTAGGG (sodium), a inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. FITC-labeled ODN TTAGGG (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

HY-P10208

RKH	Antagonist
PKH is a TLR4 antagonist. PKH is a novel tripeptide and can be isolated from Akkermansia muciniphila. RKH reduces sepsis-induced inflammatory cell activation and proinflammatory factor overproduction.

HY-150738B

FITC-labeled ODN 2088 sodium	Antagonist
FITC-labeled ODN 2088 (sodium) is a potent TLR3, TLR7 and TLR9 inhibitor. FITC-labeled ODN 2088 (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

HY-145886

TLR7/8 antagonist 1	Antagonist
TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC₅₀s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders.

HY-N0795R

Procyanidin B1 (Standard)	Antagonist
Procyanidin B1 (Standard) is the analytical standard of Procyanidin B1. This product is intended for research and analytical applications. Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.

HY-118984

CRX-526	Antagonist
CRX-526 is a TLR4 antagonist that can block the interaction of lipopolysaccharide (LPS, HY-D1056) with the immune system, including preventing the expression of pro-inflammatory genes stimulated by LPS, as well as blocking the release of TNF-α induced by LPS. CRX-526 exhibits anti-inflammatory effects in two mouse models of colitis (namely, the dextran sodium sulfate-induced colitis model and the multidrug resistance gene 1a-deficient mouse model).

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