Cat. No.: HY-11109

Resatorvid

(Synonyms: TAK-242; CLI-095)

524 Cited Publications

Customer Review

Based on 524 publication(s) in Google Scholar

Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC_50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.

For research use only. We do not sell to patients.

Purity: 98.31%
CAS No.: 243984-11-4
Formula: C₁₅H₁₇ClFNO₄S
Molecular Weight:361.82

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Resatorvid Chemical Structure

CAS No.: 243984-11-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (524)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

TLR4

TNF-R

1.9 nM (IC₅₀)

IL-6

1.3 nM (IC₅₀)

All Toll-like Receptor (TLR) Isoforms :

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC₅₀	1.3 nM Compound: (R)-(+)-5n	Inhibition of LPS-induced IL6 production in mouse RAW264.7 cells by ELISA Inhibition of LPS-induced IL6 production in mouse RAW264.7 cells by ELISA	[PMID: 16279805]
RAW264.7	IC₅₀	1.8 nM Compound: (R)-(+)-5n	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells	[PMID: 16279805]
RAW264.7	IC₅₀	1.9 nM Compound: (R)-(+)-5n	Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells by ELISA Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells by ELISA	[PMID: 16279805]

In Vitro

Resatorvid suppresses the production of NO, TNF-α, and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC₅₀ values from 11 to 33 nM^[1].
Resatorvid (1-100 nM; 4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells^[1].
Resatorvid (1-100 nM; 15 minutes; PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2), p38, and JNK/SAPK as well as degradation of IκBβ at a concentration of 100 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[1]

Cell Line:

RAW264.7 cells
Concentration:

1 nM, 10 nM, 100 nM
Incubation Time:

4 hours
Result:

TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100 nM.

Western Blot Analysis^[1]

Cell Line:

PBMCs cells
Concentration:

1 nM, 10 nM, 100 nM
Incubation Time:

15 minutes
Result:

The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner.

In Vivo

Resatorvid (TAK-242; 3 mg/kg; intraperitoneal injection; for 2 days; male C57BL/6 mice) pretreatment markedly and significantly reverses the LPS-induced body weight loss, TA muscle loss, and muscle strength loss. TAK-242 reverses the LPS-induced shrinkage of muscle fibres and increases the interstitial space. TAK-242 blocks systemic catabolic cytokine release and skeletal muscle proteolysis in LPS-administered mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6 mice (8-12 weeks of age) treated with lipopolysaccharide (LPS)^[3]
Dosage:

3 mg/kg
Administration:

Intraperitoneal injection; for 2 days
Result:

Pretreatment of mice reduced or reversed all the detrimental effects of LPS.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 243984-11-4
Appearance Solid
Molecular Weight 361.82
Formula C₁₅H₁₇ClFNO₄S
Color Off-white to yellow
SMILES

O=S([C@H]1C(C(OCC)=O)=CCCC1)(NC2=CC=C(C=C2Cl)F)=O
Synonyms

TAK-242; CLI-095
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (524)

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Journal Impact Factor

Signal Transduct Target Ther

Targeting coronaviral inflammation: aptamer-based strategies for emerging threats. [Abstract]

2026 Feb 13;11(1):54. PMID: 41680122
Signal Transduct Target Ther

SARS-CoV-2 envelope protein impairs airway epithelial barrier function and exacerbates airway inflammation via increased intracellular Cl- concentration. [Abstract]

2024 Mar 25;9(1):74. PMID: 38528022

Resatorvid purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Mar 25;9(1):74. [Abstract]

Resatorvid (5 μM; 12 h) significantly reduces E protein (50 μg/mL; 12 h)-stimulated JNK phosphorylation levels in BEAS-2B cells.
Nature

Tumour extracellular vesicles and particles induce liver metabolic dysfunction. [Abstract]

2023 Jun;618(7964):374-382. PMID: 37225988

Resatorvid purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7964):374-382. [Abstract]

qRT-PCR analysis of Tnf expression in KCs from naïve C57BL/6 mice treated with DMSO or the Tlr4 inhibitor TAK (5 μM) for 1 h followed by vehicle (100% ethanol diluted into PA-carrier medium at 1:1000 dilution) or 200 μM of PA with or without TAK (Resatorvid) (5 μM) for 4 h. n=3 mice per group.
Imeta

Akkermansia muciniphila-derived hypoacylated rough-type lipopolysaccharides alleviate diet-induced obesity via activation of TLR4-IL-23-IL-22 immune axis. [Abstract]

2025 Jul 17;4(5):e70066. PMID: 41112049
Immunity

Palmitic acid reprograms neutrophils to compromise vascular integrity and promote breast cancer lung metastasis. [Abstract]

2026 Jul 14;59(7):1964-1981.e9. PMID: 42034064
Exploration

A Bioorthogonal and Programmable Bacterial Delivery System for Spatiotemporally Targeted Therapy of Solid Tumors. [Abstract]

2025 Dec 18;5(6):20240396. PMID: 41476656
Adv Mater

Manganese@Albumin Nanocomplex and Its Assembled Nanowire Activate TLR4-Dependent Signaling Cascades of Macrophages. [Abstract]

2024 Feb;36(5):e2310979. PMID: 37994277

Resatorvid purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Feb;36(5):e2310979. [Abstract]

Gene expression of TNF-α, iNOS, IL-6, IL-1β, CCL2, IFN-β, and CXCL10 in RAW264.7 cells stimulated with 100 ng/mL LPS, 25 ng/ml IFN-γ, and TAK-242 between 10−100 nmol/L for 6 h (n = 3 biologically independent samples).

Resatorvid purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Feb;36(5):e2310979. [Abstract]

Immunoblotting images of protein expression in RAW 264.7 cells treated with 100 μg/mL BSA, 8 × 10-2 μg/mL Mn2+, or 100 μg/mL Mn@BSA NCs with (or without) adding 50 nmol/L TAK-242 inhibitor for 6 h, respectively, including MyD88, TRIF, NF-κB, IRF7, p−NFκB, and p−IRF7. Right panel, relative production quantified by Gel-Pro Analyzer 3.0 software (n= 3 biologically independent samples).
Nat Metab

The PI3K pathway preserves metabolic health through MARCO-dependent lipid uptake by adipose tissue macrophages. [Abstract]

2020 Dec;2(12):1427-1442. PMID: 33199895
Nat Biomed Eng

Biomaterial-mediated modulation of oral microbiota synergizes with PD-1 blockade in mice with oral squamous cell carcinoma. [Abstract]

2022 Jan;6(1):32-43. PMID: 34750535
Gut

Cross-talk between the gut microbiota and monocyte-like macrophages mediates an inflammatory response to promote colitis-associated tumourigenesis. [Abstract]

2020 Oct 29;70(8):1495-1506. PMID: 33122176
Cell Host Microbe

Induction of alarmin S100A8/A9 mediates activation of aberrant neutrophils in the pathogenesis of COVID-19. [Abstract]

2021 Feb 10;29(2):222-235.e4. PMID: 33388094

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2021 Feb 10;29(2):222-235.e4. [Abstract]

Resatorvid (50 μg/day; i.p.) inhibits S100a8 and Ly6g expression and viral replication in the lungs of mice infected with SARS-CoV-2 or MHV.
Cancer Res

Acetylation of CCAR2 Establishes a BET/BRD9 Acetyl Switch in Response to Combined Deacetylase and Bromodomain Inhibition. [Abstract]

2019 Mar 1;79(5):918-927. PMID: 30643017
Cancer Res

Doxorubicin-Induced Systemic Inflammation Is Driven by Upregulation of Toll-Like Receptor TLR4 and Endotoxin Leakage. [Abstract]

2016 Nov 15;76(22):6631-6642. PMID: 27680684
Adv Funct Mater

2025 Aug 3.
Autophagy

Enhanced autophagy drives endothelial tight junction loss, BBB disruption, and behavioral deficits during inflammation. [Abstract]

2026 Apr 25:1-18. PMID: 42003242
Nat Commun

TcpC inhibits neutrophil extracellular trap formation by enhancing ubiquitination mediated degradation of peptidylarginine deiminase 4. [Abstract]

2021 Jun 9;12(1):3481. PMID: 34108482
Nat Commun

A small secreted protein triggers a TLR2/4-dependent inflammatory response during invasive Candida albicans infection. [Abstract]

2019 Mar 4;10(1):1015. PMID: 30833559
Redox Biol

FGF21 alleviates adipose stem cell senescence via CD90 glycosylation-dependent glucose influx in remodeling healthy white adipose tissue. [Abstract]

2023 Nov:67:102877. PMID: 37690164
Gut Microbes

Spermidine improves gut barrier integrity and gut microbiota function in diet-induced obese mice. [Abstract]

2020 Nov 9;12(1):1-19. PMID: 33151120
J Nanobiotechnology

Succinate exacerbates mastitis in mice via extracellular vesicles derived from the gut microbiota: a potential new mechanism for mastitis. [Abstract]

2024 Nov 15;22(1):712. PMID: 39543623
Microbiome

Gut microbiota-derived metabolites mediate the neuroprotective effect of melatonin in cognitive impairment induced by sleep deprivation. [Abstract]

2023 Jan 31;11(1):17. PMID: 36721179
Acta Pharm Sin B

Gastrin attenuates sepsis-induced myocardial dysfunction by down-regulation of TLR4 expression in macrophages. [Abstract]

2023 Sep;13(9):3756-3769. PMID: 37719375
Genes Dis

FTO-mediated m6A modification alleviates autoimmune uveitis by regulating microglia phenotypes via the GPC4/TLR4/NF-κB signaling axis. [Abstract]

2022 Oct 4;10(5):2179-2193. PMID: 37492748
Interdiscip Med

2026 May 18.
J Clin Invest

Lysosomal exocytosis of HSP70 stimulates monocytic BMP6 expression in Sjögren's syndrome. [Abstract]

2022 Mar 15;132(6):e152780. PMID: 35113815
Adv Sci (Weinh)

OTUD6A in Airway Epithelial Cells Exacerbates Allergic Asthma by Promoting Airway Inflammation and Airway Remodeling Through Deubiquitination of hResistin/mRELMα. [Abstract]

2026 Jan 20:e16355. PMID: 41560298
Adv Sci (Weinh)

Rescuing Mitochondrial Dysfunction in Macrophages Prevents Osteonecrosis of the Jaw in Anti-Resorptive Therapy. [Abstract]

2025 Dec 7:e17586. PMID: 41354629
Adv Sci (Weinh)

Deciphering the Role and Mechanism of Decidual Monocyte-Derived Macrophage Infiltration in Obstetric Antiphospholipid Syndrome at Single-Cell Resolution. [Abstract]

2025 Aug 7:e03480. PMID: 40776470
Adv Sci (Weinh)

Neutrophil Mobilization Triggers Microglial Functional Change to Exacerbate Cerebral Ischemia-Reperfusion Injury. [Abstract]

2025 Jun 25:e03722. PMID: 40557450
Cell Rep Med

A CD36-dependent non-canonical lipid metabolism program promotes immune escape and resistance to hypomethylating agent therapy in AML. [Abstract]

2024 May 29:101592. PMID: 38843841
Biomaterials

Ultrasound-responsive renal-targeted nanoparticles deliver TAK-242 to inhibit NF-κB/NLRP3 signaling and attenuate sepsis-associated acute kidney injury. [Abstract]

2025 Dec 14:329:123922. PMID: 41481962
Biomaterials

Cholesterol-modified DP7 enhances the effect of individualized cancer immunotherapy based on neoantigens. [Abstract]

2020 May;241:119852. PMID: 32120313
Biomaterials

Ex-vivo generation of drug-eluting islets improves transplant outcomes by inhibiting TLR4-Mediated NFkB upregulation. [Abstract]

2018 Mar;159:13-24. PMID: 29309990
Carbohydr Polym

Structural analysis and immunomodulatory properties of lipopolysaccharide from the gut symbiont Phocaeicola dorei. [Abstract]

2026 Feb 1:373:124566. PMID: 41320355
Carbohydr Polym

Innate immune receptors co-recognition of polysaccharides initiates multi-pathway synergistic immune response. [Abstract]

2023 Apr 1:305:120533. PMID: 36737186
Carbohydr Polym

Immunoregulatory properties of the cultivated Artemisia rupestris L. polysaccharide as a potential adjuvant. [Abstract]

2022 Sep 1:291:119525. PMID: 35698367
Carbohydr Polym

A purified acidic polysaccharide from Sarcandra glabra as vaccine adjuvant to enhance anti-tumor effect of cancer vaccine. [Abstract]

2021 Jul 1:263:117967. PMID: 33858570
Carbohydr Polym

Chitosan oligosaccharide-mediated attenuation of LPS-induced inflammation in IPEC-J2 cells is related to the TLR4/NF-κB signaling pathway. [Abstract]

2019 Sep 1;219:269-279. PMID: 31151525
Carbohydr Polym

Structural characterization and macrophage activation of a hetero-galactan isolated from Flammulina velutipes. [Abstract]

2018 Mar 1;183:207-218. PMID: 29352876

Resatorvid purchased from MedChemExpress. Usage Cited in: Carbohydr Polym. 2018 Mar 1;183:207-218. [Abstract]

TAK-242 significantly reduces the protein expression of p-JNK, p-ERK, p-p38, p-Akt and LC3-II.
Chem Eng J

2023 Oct 15, 474, 145318.
J Control Release

Fibrin gel-based co-delivery of self-adjuvant tumor vaccine and PD-1 blockade for post-surgical gastric cancer immunotherapy. [Abstract]

2026 Mar 10:391:114629. PMID: 41544668
J Control Release

Silver nanoclusters show advantages in macrophage tracing in vivo and modulation of anti-tumor immuno-microenvironment. [Abstract]

2022 Aug:348:470-482. PMID: 35691499
Cell Mol Biol Lett

A frog peptide provides new strategies for the intervention against skin wound healing. [Abstract]

2023 Jul 28;28(1):61. PMID: 37501100
Pharmacol Res

Losartan attenuates sepsis-induced cardiomyopathy by regulating macrophage polarization via TLR4-mediated NF-κB and MAPK signaling. [Abstract]

2022 Sep 28;185:106473. PMID: 36182039
Pharmacol Res

TLR4 and AT1R mediate blood-brain barrier disruption, neuroinflammation, and autonomic dysfunction in spontaneously hypertensive rats. [Abstract]

2021 Oct 2;105877. PMID: 34610452
Cell Death Dis

Neutrophil extracellular traps impair intestinal barrier functions in sepsis by regulating TLR9-mediated endoplasmic reticulum stress pathway. [Abstract]

2021 Jun 11;12(6):606. PMID: 34117211
Small

ROS Responsive Cerium Oxide Biomimetic Nanoparticles Alleviates Calcium Oxalate Crystals Induced Kidney Injury via Suppressing Oxidative Stress and M1 Macrophage Polarization. [Abstract]

2024 Dec 4:e2405417. PMID: 39629501
Int J Biol Sci

BGN/FAP/STAT3 positive feedback loop mediated mutual interaction between tumor cells and mesothelial cells contributes to peritoneal metastasis of gastric cancer. [Abstract]

2023 Jan 1;19(2):465-483. PMID: 36632455
Cell Commun Signal

NETs activate the GAS6-AXL-NLRP3 axis in macrophages to drive morphine tolerance. [Abstract]

2025 Apr 11;23(1):181. PMID: 40217343

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Apr 11;23(1):181. [Abstract]

BMDMs were pretreated with a TLR2 inhibitor (C29; HY-100461; 10 µM), TLR4 inhibitor (TAK242; HY-11109; 10 µM), TLR7 inhibitor (IRS661, 1 µM), TLR8 inhibitor (CU-CPT9a; HY-112667; 10 µM), or TLR9 inhibitor (IRS869, 1 µM) for 1 h, and then treated with NETs (500 ng/mL) for 3 h. The levels of Il1b, Il6 were measured by qPCR (n = 6).

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Apr 11;23(1):181. [Abstract]

BMDMs were pretreated with a TLR2 inhibitor (C29; HY-100461; 10 µM), TLR4 inhibitor (TAK242; HY-11109; 10 µM), TLR7 inhibitor (IRS661, 1 µM), TLR8 inhibitor (CU-CPT9a; HY-112667; 10 µM), or TLR9 inhibitor (IRS869, 1 µM) for 1 h, and then treated with NETs (500 ng/mL) for 3 h. The level of Tnfa mRNA was measured by qPCR (n = 6).
J Neuroinflammation

α-Synuclein disrupts microglial autophagy through STAT1-dependent suppression of Ulk1 transcription. [Abstract]

2024 Oct 26;21(1):275. PMID: 39462396
J Neuroinflammation

Regulatory T cells alleviate myelin loss and cognitive dysfunction by regulating neuroinflammation and microglial pyroptosis via TLR4/MyD88/NF-κB pathway in LPC-induced demyelination. [Abstract]

2023 Feb 18;20(1):41. PMID: 36803990
J Neuroinflammation

Thymosin β4 reverses phenotypic polarization of glial cells and cognitive impairment via negative regulation of NF-κB signaling axis in APP/PS1 mice. [Abstract]

2021 Jun 28;18(1):146. PMID: 34183019
J Neuroinflammation

Hippocampal Mrp8/14 signaling plays a critical role in the manifestation of depressive-like behaviors in mice. [Abstract]

2018 Sep 4;15(1):252. PMID: 30180864

Resatorvid purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Sep 4;15(1):252. [Abstract]

The phosphorylation of NF-κB p65 evoked by Mrp14 is decreased after TAK-242 treatment.
Phytomedicine

Ferulic acid ameliorates TLR4-mediated macrophage activation by irreversibly binding to peroxiredoxin 1 to inhibit its dimerization and secretion. [Abstract]

2025 Sep 12:148:157254. PMID: 40966782
Phytomedicine

Qing-Fei-Pai-Du-Tang ameliorates lipopolysaccharide-induced rat acute lung injury through attenuating pulmonary microcirculatory disturbances via multi-target regulation. [Abstract]

2025 May 12:143:156839. PMID: 40412059
Phytomedicine

Integrated transcriptomics and network pharmacology to reveal the mechanism of Physochlainae Radix in the treatment of asthma. [Abstract]

2025 Feb 6:139:156470. PMID: 39947003
Phytomedicine

Rice bran active peptide (RBAP) inhibited macrophage differentiation to foam cell and atherosclerosis in mice via regulating cholesterol efflux. [Abstract]

2024 Jul 14:132:155864. PMID: 39032281
Phytomedicine

Pentoxifylline attenuates nonalcoholic fatty liver by inhibiting hepatic macrophage polarization to the M1 phenotype. [Abstract]

2022 Nov:106:154368. PMID: 35994850
J Pharm Anal

Dihydroartemisinin ameliorates innate inflammatory response induced by Streptococcussuis-derived muramidase-released protein via inactivation of TLR4-dependent NF-κB signaling. [Abstract]

2023 Oct;13(10):1183-1194. PMID: 38024861
EBioMedicine

Neutrophil extracellular traps as a unique target in the treatment of chemotherapy-induced peripheral neuropathy. [Abstract]

2023 Apr:90:104499. PMID: 36870200
EBioMedicine

F. nucleatum facilitates oral squamous cell carcinoma progression via GLUT1-driven lactate production. [Abstract]

2023 Feb:88:104444. PMID: 36709580
EBioMedicine

Toll-like receptor 2 and Toll-like receptor 4 exhibit distinct regulation of cancer cell stemness mediated by cell death-induced high-mobility group box 1. [Abstract]

2019 Feb:40:135-150. PMID: 30679086
EBioMedicine

Prosaposin promotes the proliferation and tumorigenesis of glioma through toll-like receptor 4 (TLR4)-mediated NF-κB signaling pathway. [Abstract]

2018 Nov:37:78-90. PMID: 30385233

Resatorvid purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Nov:37:78-90. [Abstract]

TAK-242 alters NF-κB downstream targets in PSAP overexpressing SNB19 and GSC-21 cells as measured by western blotting.
J Hazard Mater

Role of macrophage AHR/TLR4/STAT3 signaling axis in the colitis induced by non-canonical AHR ligand aflatoxin B1. [Abstract]

2023 Jun 15:452:131262. PMID: 36989784
Cell Death Discov

NINJ1-mediated plasma membrane rupture of pyroptotic endothelial cells exacerbates blood-brain barrier destruction caused by neutrophil extracellular traps in traumatic brain injury. [Abstract]

2025 Feb 20;11(1):69. PMID: 39979243
Cell Death Discov

FN-EDA mediates angiogenesis of hepatic fibrosis via integrin-VEGFR2 in a CD63 synergetic manner. [Abstract]

2020 Dec 8;6(1):140. PMID: 33293521
Diabetologia

Extracellular HMGB1 exacerbates autoimmune progression and recurrence of type 1 diabetes by impairing regulatory T cell stability. [Abstract]

2020 May;63(5):987-1001. PMID: 32072192
J Crohns Colitis

Intestinal adipocytes transdifferentiate into myofibroblast-like cells and contribute to fibrosis in Crohn's disease. [Abstract]

2024 Aug 14;18(8):1292-1304. PMID: 38466138
NPJ Sci Food

Long-term sucralose exposure accelerates ovarian aging via gut microbiota dysbiosis. [Abstract]

2026 Mar 24. PMID: 41876529
J Transl Med

Exploring the role of cellular plasticity in metabolic dysfunction-associated steatosis and related molecular mechanisms. [Abstract]

2025 Nov 13;23(1):1278. PMID: 41233849
J Transl Med

Gut microbiota dysbiosis exacerbates heart failure by the LPS-TLR4/NF-κB signalling axis: mechanistic insights and therapeutic potential of TLR4 inhibition. [Abstract]

2025 Jul 10;23(1):762. PMID: 40640887
Sci China Life Sci

Unveiling the choroidal immune landscape revealed interferon-gamma and TNF-alpha as novel therapeutic targets in dry AMD. [Abstract]

2025 Oct 10. PMID: 41077603
Anesthesiology

Morphine Exacerbates Postfracture Nociceptive Sensitization, Functional Impairment, and Microglial Activation in Mice. [Abstract]

2019 Feb;130(2):292-308. PMID: 30418215

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

Detection of PCNA by western blotting with the treatment of 2DG, MET and COM.

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

Detection of PCNA by immunohistochemistry with the treatment of 2DG, MET and COM.

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

The detection of cell cycle-related proteins by western blotting with the treatment of 2DG, MET and COM.

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

Detection of activated signaling molecules in the mTOR pathway via western blotting with the treatment of 2DG, MET and COM.

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

The detection of activated signaling molecules of the ERK pathway via western blotting with the treatment of 2DG, MET and COM.

Resatorvid purchased from MedChemExpress. Usage Cited in: Anesthesiology. 2019 Feb;130(2):292-308. [Abstract]

Detection of the expression of key glucose metabolism enzymes via western blotting with the treatment of 2DG, MET and COM.
Diabetes

mtDNA Haplogroup N9a Increases the Risk of Type 2 Diabetes by Altering Mitochondrial Function and Intracellular Mitochondrial Signals. [Abstract]

2018 Jul;67(7):1441-1453. PMID: 29735607
Food Chem X

Comparative analysis of pectic polysaccharides isolated from various thinned young red-fleshed kiwifruits: Structural properties and biological functions. [Abstract]

2025 Jun 29:29:102709. PMID: 40677549
Food Chem X

The degree of esterification influences the bioactivity of pectic polysaccharides isolated from Lithocarpus litseifolius. [Abstract]

2025 Apr 12:27:102462. PMID: 40297662
J Eur Acad Dermatol Venereol

Recombinant Treponema pallidum protein Tp0136 promotes fibroblast migration by modulating MCP-1/CCR2 through TLR4. [Abstract]

2020 Apr;34(4):862-872. PMID: 31856347
Osteoarthritis Cartilage

Low back pain and disc degeneration are decreased following chronic toll-like receptor 4 inhibition in a mouse model. [Abstract]

2018 Sep;26(9):1236-1246. PMID: 29908959
Basic Res Cardiol

MD2 mediates angiotensin II-induced cardiac inflammation and remodeling via directly binding to Ang II and activating TLR4/NF-κB signaling pathway. [Abstract]

2017 Jan;112(1):9. PMID: 28013347
Chin Med J (Engl)

Toll-like Receptor 4 Signaling Pathway in the Protective Effect of Pioglitazone on Experimental Immunoglobulin A Nephropathy. [Abstract]

2017 Apr 20;130(8):906-913. PMID: 28397719

Resatorvid purchased from MedChemExpress. Usage Cited in: Chin Med J (Engl). 2017 Apr 20;130(8):906-913. [Abstract]

The levels of TLR4, IL-1β mRNA, and protein in TAK242 group are much lower than those in IgAN_TAK242 group.
Food Res Int

Potential structure-function relationships of pectic polysaccharides from quinoa microgreens: Impact of various esterification degrees. [Abstract]

2024 Jul:187:114395. PMID: 38763655
Food Res Int

Mechanisms of RAW264.7 macrophages immunomodulation mediated by polysaccharide from mung bean skin based on RNA-seq analysis. [Abstract]

2022 Apr:154:111017. PMID: 35337574
Int J Biol Macromol

Portulaca oleracea polysaccharide alleviates UVB-induced solar dermatitis in association with macrophage immunomodulation. [Abstract]

2026 Jun 11:152898. PMID: 42276470
Int J Biol Macromol

2026 May 29;370:152795.
Int J Biol Macromol

Isolation, structural characterization and immunoregulatory activity of a novel acidic polysaccharide from Ganoderma sinense. [Abstract]

2026 Mar 3:151196. PMID: 41786176
Int J Biol Macromol

A glycoprotein UGP2A from the medicinal insect Ulomoides dermestoides alleviates deep vein thrombosis via the TLR4/MyD88 signaling pathway. [Abstract]

2026 Feb;341(Pt 1):150216. PMID: 41547510
Int J Biol Macromol

Two pectic polysaccharides from Stemona tuberosa Lour. roots with detailed structural features display potent immunoenhancing activity via TLR signaling pathway. [Abstract]

2026 Jan;340(Pt 1):150166. PMID: 41519324
Int J Biol Macromol

2025 Dec 31.
Int J Biol Macromol

Longan polysaccharides promote Th1 and Treg cell differentiation via dendritic cells. [Abstract]

2025 Sep;321(Pt 3):146462. PMID: 40749906
Int J Biol Macromol

An alkali-extracted acidic heteropolysaccharide from Portulaca oleracea L. ameliorates acute lung injury in septic mice by inhibiting macrophage pyroptosis. [Abstract]

2025 Jul;318(Pt 2):145139. PMID: 40505906
J Headache Pain

Inhibition of S100A4 decreases neurotoxic astrocyte reactivity and attenuates neuropathic pain via the TLR4/NF-κB pathway in a rat model of spinal nerve ligation. [Abstract]

2025 May 1;26(1):97. PMID: 40312684
Int J Biol Macromol

Anti-inflammatory effect of polysaccharides from Sambucus williamsii Hance roots in lipopolysaccharide-stimulated RAW264.7 macrophages and acute lung injury in mice. [Abstract]

2025 May;306(Pt 1):141368. PMID: 39988171
Int J Biol Macromol

Inhibition of lncEPS by TLR4/NF-κB pathway induces ventilator-induced lung injury by decreasing its binding to and upregulating Hspa5. [Abstract]

2024 Nov 29:138238. PMID: 39617220
Int J Biol Macromol

Camellia sinensis polysaccharide attenuates inflammatory responses via the ROS-mediated pathway by endocytosis. [Abstract]

2024 May;267(Pt 2):131674. PMID: 38641285
Int J Biol Macromol

Structure of a polysaccharide MDP2-1 from Melastoma dodecandrum Lour. and its anti-inflammatory effects. [Abstract]

2024 Apr;265(Pt 2):131015. PMID: 38521298
Int J Biol Macromol

Molecular mechanisms of macrophage immunomodulation mediated by Areca inflorescence polysaccharides based on RNA-seq analysis. [Abstract]

2024 Apr;263(Pt 1):130076. PMID: 38354932
Int J Biol Macromol

Strongylocentrotus nudus egg polysaccharide (SEP) suppresses HBV replication via activation of TLR4-induced immune pathway. [Abstract]

2023 Aug 1:245:125539. PMID: 37355064
Int J Biol Macromol

Structural characterization and immunomodulatory activity of an arabinogalactan from Jasminum sambac (L.) Aiton tea processing waste. [Abstract]

2023 Apr 30:235:123816. PMID: 36841385
Int J Biol Macromol

Evaluation and mechanism of immune enhancement effects of Pleurotus ferulae polysaccharides-gold nanoparticles. [Abstract]

2023 Feb 1:227:1015-1026. PMID: 36460244
Int J Biol Macromol

CRM197-conjugated multi antigen dominant epitope for effective human cytomegalovirus vaccine development. [Abstract]

2023 Jan 1:224:79-93. PMID: 36252620
Int J Biol Macromol

Fucoidan, as an immunostimulator promotes M1 macrophage differentiation and enhances the chemotherapeutic sensitivity of capecitabine in colon cancer. [Abstract]

2022 Dec 1;222(Pt A):562-572. PMID: 36170928
Int J Biol Macromol

Influence of glycosyl composition on the immunological activity of pectin and pectin-derived oligosaccharide. [Abstract]

2022 Dec 1;222(Pt A):671-679. PMID: 36174858
Int J Biol Macromol

The immunomodulatory activity of degradation products of Sesbania cannabina galactomannan with different molecular weights. [Abstract]

2022 Apr 30:205:530-538. PMID: 35217078
BMC Med

HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]

2021 Oct 15;19(1):247. PMID: 34649530
Int J Biol Macromol

Immunomodulatory effect of intracellular polysaccharide from mycelia of Agaricus bitorquis (QuéL.) Sacc. Chaidam by TLR4-mediated MyD88 dependent signaling pathway. [Abstract]

2021 Jul 31:183:79-89. PMID: 33901556
Int J Biol Macromol

Apple polysaccharide prevents from colitis-associated carcinogenesis through regulating macrophage polarization. [Abstract]

2020 Oct 15;161:704-711. PMID: 32544579
Int J Biol Macromol

Preparation and evaluation of the adjuvant effect of curdlan sulfate in improving the efficacy of dendritic cell-based vaccine for antitumor immunotherapy. [Abstract]

2020 Mar 1;146:273-284. PMID: 31904453
Int J Biol Macromol

Cordyceps militaris polysaccharide converts immunosuppressive macrophages into M1-like phenotype and activates T lymphocytes by inhibiting the PD-L1/PD-1 axis between TAMs and T lymphocytes. [Abstract]

2020 May 1;150:261-280. PMID: 32044366
Int J Biol Macromol

Potential immunomodulatory activities of a lectin from the mushroom Latiporus sulphureus. [Abstract]

2019 Jun 1:130:399-406. PMID: 30822473
Int J Biol Macromol

Polysaccharide from Phellinus Igniarius activates TLR4-mediated signaling pathways in macrophages and shows immune adjuvant activity in mice. [Abstract]

2019 Feb 15:123:157-166. PMID: 30439422
Int J Biol Macromol

Study on the immunomodulatory activity of a novel polysaccharide from the lichen Umbilicaria Esculenta. [Abstract]

2019 Jan:121:846-851. PMID: 30339998
Int J Biol Macromol

Polysaccharide isolated from Sarcodon aspratus induces RAW264.7 activity via TLR4-mediated NF-κB and MAPK signaling pathways. [Abstract]

2018 Dec;120(Pt A):1039-1047. PMID: 30171950
Int J Biol Macromol

Polygonatum sibiricum polysaccharides play anti-cancer effect through TLR4-MAPK/NF-κB signaling pathways. [Abstract]

2018 May:111:813-821. PMID: 29343453
Int J Biol Macromol

Macrophage immunomodulatory activity of the polysaccharide isolated from Collybia radicata mushroom. [Abstract]

2018 Mar:108:300-306. PMID: 29222012
NPJ Parkinsons Dis

LRRK2R1627P mutation amplifies environmental risk factors induced chronic inflammation and α-synuclein aggregation in the gut of rats. [Abstract]

2026 Feb 7;12(1):68. PMID: 41654526
Neural Regen Res

Porcine decellularized nerve matrix hydrogel attenuates neuroinflammation after peripheral nerve injury by inhibiting the TLR4/MyD88/NF-κB axis. [Abstract]

2026 Mar 1;21(3):1222-1235. PMID: 39589179
Neural Regen Res

Suppressing high mobility group box-1 release alleviates morphine tolerance via the adenosine 5'-monophosphate-activated protein kinase/heme oxygenase-1 pathway. [Abstract]

2023 Sep;18(9):2067-2074. PMID: 36926733
EMBO J

Erythropoietin signaling in peripheral macrophages is required for systemic β-amyloid clearance. [Abstract]

2022 Nov 17;41(22):e111038. PMID: 36215698
Mol Med

Evobrutinib mitigates neuroinflammation after ischemic stroke by targeting M1 microglial polarization via the TLR4/Myd88/NF-κB pathway. [Abstract]

2025 Apr 22;31(1):148. PMID: 40263985
Cell Mol Gastroenterol Hepatol

Kupffer Cell-Derived Exosomal S100A8/A9 Promotes Inflammasome-Dependent Pyroptotic Lung Injury in Acute Pancreatitis. [Abstract]

2026 May 12:101810. PMID: 42128052
Free Radic Biol Med

SIRT4 knockout exacerbates lung injury in septic mice by activating TLR4/MYD88/NFκB pathway. [Abstract]

2025 Dec 11:244:229-237. PMID: 41389851
Cancer Immunol Res

NET-Triggered NLRP3 Activation and IL18 Release Drive Oxaliplatin-Induced Peripheral Neuropathy. [Abstract]

2022 Dec 2;10(12):1542-1558. PMID: 36255412
J Anim Sci Biotechnol

Overexpression of Toll-like receptor 4 contributes to the internalization and elimination of Escherichia coli in sheep by enhancing caveolae-dependent endocytosis. [Abstract]

2021 May 10;12(1):63. PMID: 33966642
ACS Appl Mater Interfaces

Effective Radiotherapy in Tumor Assisted by Ganoderma lucidum Polysaccharide-Conjugated Bismuth Sulfide Nanoparticles through Radiosensitization and Dendritic Cell Activation. [Abstract]

2019 Aug 7;11(31):27536-27547. PMID: 31294958
Cell Rep

Divergent toxicity mechanisms of amyloid-beta aggregates arising from a single aggregation reaction. [Abstract]

2026 Jun 22;45(7):117595. PMID: 42329766
Cell Rep

Microglial macrophage-derived ds-HMGB1 in DRG orchestrates neuropathic pain through immune-neural signaling. [Abstract]

2025 Dec 10;44(12):116671. PMID: 41385369
Cell Rep

Alveolar macrophages critically control infection by seasonal human coronavirus OC43 to avoid severe pneumonia. [Abstract]

2025 Apr 11;44(4):115531. PMID: 40222012
Cell Rep

Bladder epithelial cell phosphate transporter inhibition protects mice against uropathogenic Escherichia coli infection. [Abstract]

2022 Apr 19;39(3):110698. PMID: 35443182
Br J Pharmacol

Toll-like receptor 4 mediates lipopolysaccharide-induced emesis. [Abstract]

2026 Aug;183(16):4592-4609. PMID: 42063347
J Ginseng Res

Ginsenoside Rg5 modulates the TLR4 and BCL-2 pathways by inhibiting NOX1, thereby alleviating inflammation, apoptosis and pyroptosis in hyperuricemia nephropathy. [Abstract]

2025 Jul;49(4):426-437. PMID: 40621077
Brain Behav Immun

Innate immune system signaling and intestinal dendritic cells migration to the brain underlie behavioral changes after microbial colonization in adult mice. [Abstract]

2025 Jul:127:238-250. PMID: 40068794
Brain Behav Immun

Ds-HMGB1 and fr-HMGB induce depressive behavior through neuroinflammation in contrast to nonoxid-HMGB1. [Abstract]

2017 Jan:59:322-332. PMID: 27647532
Chin Med

Dachaihu decoction alleviates septic liver injury by modulating the intestinal barrier dysfunction and suppressing the NF-κB/NLRP3/Caspase-1 signaling pathway. [Abstract]

2026 Jun 16;21(1):168. PMID: 42298689
Chin Med

Fuzheng Jiedu formula attenuates acute pneumonia by coordinated regulation of macrophage NLRP3 inflammasome and neutrophil NETs. [Abstract]

2026 Jan 4;21(1):1. PMID: 41484909
Chin Med

Oleuropein alleviates myocardial ischemia-reperfusion injury by suppressing oxidative stress and excessive autophagy via TLR4/MAPK signaling pathway. [Abstract]

2024 Apr 8;19(1):59. PMID: 38589925
Cell Mol Neurobiol

Blockage of TRPV4 Downregulates the Nuclear Factor-Kappa B Signaling Pathway to Inhibit Inflammatory Responses and Neuronal Death in Mice with Pilocarpine-Induced Status Epilepticus. [Abstract]

2023 Apr;43(3):1283-1300. PMID: 35840809
Int J Oncol

S100A8 facilitates cholangiocarcinoma metastasis via upregulation of VEGF through TLR4/NF‑κB pathway activation. [Abstract]

2020 Jan;56(1):101-112. PMID: 31746424
Front Immunol

Toll-Like Receptor- and Protein Kinase R-Induced Type I Interferon Sustains Infection of Leishmania donovani in Macrophages. [Abstract]

2022 Jan 28:13:801182. PMID: 35154115
Front Immunol

Mannose Receptor Mediates the Activation of Chitooligosaccharides on Blunt Snout Bream ( Megalobrama amblycephala) Macrophages. [Abstract]

2021 Aug 2;12:686846. PMID: 34408745
Front Immunol

Hypoxia Exacerbates Inflammatory Acute Lung Injury via the Toll-Like Receptor 4 Signaling Pathway. [Abstract]

2018 Jul 23:9:1667. PMID: 30083155

Resatorvid purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Jul 23:9:1667. [Abstract]

The inhibitory effect of TAK-242 on the TLR4 mRNA and protein expression is detected by RT-qPCR and Western Blot in NR8383 cells.
Front Immunol

Homeobox a5 Promotes White Adipose Tissue Browning Through Inhibition of the Tenascin C/Toll-Like Receptor 4/Nuclear Factor Kappa B Inflammatory Signaling in Mice. [Abstract]

2018 Mar 29:9:647. PMID: 29651293
Front Immunol

Positive Feedback Regulation between Transglutaminase 2 and Toll-Like Receptor 4 Signaling in Hepatic Stellate Cells Correlates with Liver Fibrosis Post Schistosoma japonicum Infection. [Abstract]

2017 Dec 13:8:1808. PMID: 29321784

Resatorvid purchased from MedChemExpress. Usage Cited in: Front Immunol. 2017 Dec 13:8:1808. [Abstract]

The protein expression levels of Tgm2 in the 8-week Sj-infected mouse liver with TAK242 treatment are significantly reduced compared to those of the non-treated control.
Pharmaceutics

Cerebroprotective Effects of the TLR4-Binding DNA Aptamer ApTOLL in a Rat Model of Ischemic Stroke and Thrombectomy Recanalization. [Abstract]

2024 May 30;16(6):741. PMID: 38931862
Virulence

Neutrophil extracellular trap-borne C3-driven endothelial dysfunction in Klebsiella pneumoniae liver abscess. [Abstract]

2025 Dec;16(1):2580104. PMID: 41146461
JCI Insight

Molecular control of PDPNhi macrophage subset induction by ADAP as a host defense in sepsis. [Abstract]

2025 Feb 4:e186456. PMID: 39903516
J Ethnopharmacol

Qingda granules alleviate cerebral ischemia/reperfusion injury by inhibiting TLR4/NF-κB/NLRP3 signaling in microglia. [Abstract]

2024 Apr 24:324:117712. PMID: 38184025
J Ethnopharmacol

Zhilong Huoxue Tongyu Capsule attenuates hemorrhagic transformation through the let-7f/TLR4 signaling pathway. [Abstract]

2023 Aug 10:312:116521. PMID: 37080368
J Ethnopharmacol

Aqueous extracts from cultivated Cistanche deserticola Y.C. Ma as polysaccharide adjuvant promote immune responses via facilitating dendritic cell activation. [Abstract]

2021 Sep 15:277:114256. PMID: 34062250
J Ethnopharmacol

The flavonoid-enriched extract from the root of Smilax china L. inhibits inflammatory responses via the TLR-4-mediated signaling pathway. [Abstract]

2020 Jun 28;256:112785. PMID: 32222576
J Autoimmun

Toll-like receptor 4 antagonist TAK-242 inhibits autoinflammatory symptoms in DITRA. [Abstract]

2017 Jun:80:28-38. PMID: 28196704
J Agric Food Chem

Structure and Immunoactivity of Low Molecular Weight Pectin-Complex Decorated Diverse Oligosaccharide Domains from Roots of Platycodon grandiflorum (Jacq.) A. DC. [Abstract]

2025 Oct 21. PMID: 41118443
J Agric Food Chem

Molecular Mechanism of Glycation Structure-Mediated Immune Recognition and Sensitization by Typical Milk Allergens. [Abstract]

2025 Aug 27;73(34):21566-21577. PMID: 40801482
J Agric Food Chem

Taurine Alleviates Experimental Colitis by Enhancing Intestinal Barrier Function and Inhibiting Inflammatory Response through TLR4/NF-κB Signaling. [Abstract]

2024 May 18. PMID: 38761152
Microb Biotechnol

Peptide MSI-1 inhibited MCR-1 and regulated outer membrane vesicles to combat immune evasion of Escherichia coli. [Abstract]

2023 Sep;16(9):1755-1773. PMID: 37329166
Ecotoxicol Environ Saf

Co-exposure of microcystin-LR and nitrite induced kidney injury through TLR4/NLRP3/GSDMD-mediated pyroptosis. [Abstract]

2024 Jun 24:281:116629. PMID: 38917587
Ecotoxicol Environ Saf

Embryo injected with Ochratoxin A induced jejunum injury in ducklings by activating the TLR4 signaling pathway: Involvement of intestinal microbiota. [Abstract]

2024 Jun 29:281:116666. PMID: 38945100
Ecotoxicol Environ Saf

MiR-140-5p/TLR4 /NF-κB signaling pathway: Crucial role in inflammatory response in 16HBE cells induced by dust fall PM2.5. [Abstract]

2021 Jan 15;208:111414. PMID: 33080424
Biochem Pharmacol

A first-in-class orally available DC-SIGN agonist octaparin alleviates TNBS-induced colitis by preserving gut barrier integrity. [Abstract]

2026 Aug;250(Pt 2):118083. PMID: 42155734
Biochem Pharmacol

Ferulic acid promotes thrombopoiesis via TLR4/JAK2/STAT3 signaling: A novel therapeutic strategy for thrombocytopenia. [Abstract]

2025 Jun 24:117088. PMID: 40571222
Cell Mol Life Sci

Endothelial CD38-induced endothelial-to-mesenchymal transition is a pivotal driver in pulmonary fibrosis. [Abstract]

2024 Dec 27;82(1):30. PMID: 39725783
Life Sci

Enhanced expression of coxsackievirus and adenovirus receptor in lipopolysaccharide-induced inflammatory macrophages is through TRIF-dependent innate immunity pathway. [Abstract]

2021 Jan 15;265:118832. PMID: 33259866
Life Sci

Epigallocatechin-3-gallate alleviates paraquat-induced acute lung injury and inhibits upregulation of toll-like receptors. [Abstract]

2017 Feb 1:170:25-32. PMID: 27890776

Resatorvid purchased from MedChemExpress. Usage Cited in: Life Sci. 2017 Feb 1:170:25-32. [Abstract]

Inhibition of TLR4 signaling attenuates PQ-induced NF-B activation and cytokine production. A549 cells are pre-treated 1 M TAK-242, followed by treatment with 300 M PQ for 24 h. The levels of (A) p-IB, (B) nuclear NF-B and (C) TLR4 are examined by Western blot analysis. (D) The relative mRNA expressions of TNF-, IL-1and IL-6 are measured by real-time PCR.
Food Funct

Sodium butyrate attenuates experimental neonatal necrotizing enterocolitis by suppressing TLR4-mediated NLRP3 inflammasome-dependent pyroptosis. [Abstract]

2025 Apr 14. PMID: 40223745
Food Funct

Garlic-derived exosome-like nanovesicles alleviate dextran sulphate sodium-induced mouse colitis via the TLR4/MyD88/NF-κB pathway and gut microbiota modulation. [Abstract]

2023 Aug 14;14(16):7520-7534. PMID: 37523213
Food Funct

Sulfated Chinese yam polysaccharide enhances the immunomodulatory activity of RAW 264.7 cells via the TLR4-MAPK/NF-κB signaling pathway. [Abstract]

2022 Feb 7;13(3):1316-1326. PMID: 35037682
Food Funct

A polysaccharide extracted from alfalfa activates splenic B cells by TLR4 and acts primarily via the MAPK/p38 pathway. [Abstract]

2020 Oct 21;11(10):9035-9047. PMID: 33021613
Food Funct

Purification, characterization and bioactivities of polysaccharides from Pleurotus ferulae. [Abstract]

2017 May 24;8(5):1905-1914. PMID: 28436508
Food Biosci

2025 Sep.
Food Biosci

2025 Sep.
Food Biosci

2025 Jun.
Food Biosci

2025 Jun.
Inflamm Res

Lipopolysaccharide (LPS) induces sclerostin secretion by extracellular vesicle via TLR4/miR-92a-3p/PTEN/NF-κB signalling pathway in murine macrophage. [Abstract]

2025 Jan 25;74(1):27. PMID: 39862242
RSC Adv

Geniposide attenuates Aβ25-35-induced neurotoxicity via the TLR4/NF-κB pathway in HT22 cells. [Abstract]

2018 May 23;8(34):18926-18937. PMID: 35539637
Foods

A Polysaccharide from Ficus carica L. Exerts Immunomodulatory Activity in Both In Vitro and In Vivo Experimental Models. [Abstract]

2024 Jan 7;13(2):195. PMID: 38254496
Hepatol Commun

Aging aggravates liver fibrosis through downregulated hepatocyte SIRT1-induced liver sinusoidal endothelial cell dysfunction. [Abstract]

2023 Dec 22;8(1):e0350. PMID: 38126919
Pharm Biol

Catalpol relieved angiotensin II-induced blood-brain barrier destruction via inhibiting the TLR4 pathway in brain endothelial cells. [Abstract]

2022 Dec;60(1):2210-2218. PMID: 36369944
Oncogenesis

Tumor-derived HMGB1 induces CD62Ldim neutrophil polarization and promotes lung metastasis in triple-negative breast cancer. [Abstract]

2020 Sep 17;9(9):82. PMID: 32943604
ACS Appl Nano Mater

2026 Jun 2;9(23):11045–11063.
Commun Biol

Pentraxin 3 ameliorates glucocorticoid-induced osteonecrosis of the femoral head via TLR4/NF-κB/FGF21 signaling axis. [Abstract]

2025 Dec 2;9(1):27. PMID: 41331332
Commun Biol

MIF downregulation attenuates neuroinflammation via TLR4/MyD88/TRAF6/NF-κB pathway to protect dopaminergic neurons in Parkinson's disease model. [Abstract]

2025 Nov 18;8(1):1595. PMID: 41254084
Microb Cell Fact

TAK-242 ameliorates DSS-induced colitis by regulating the gut microbiota and the JAK2/STAT3 signaling pathway. [Abstract]

2020 Aug 6;19(1):158. PMID: 32762699
Respir Res

Activation of PBK by Gal-3 contributes to pulmonary artery hypertension by promoting PRC1 activation. [Abstract]

2026 Jan 29;27(1):65. PMID: 41612370
Eur J Pharmacol

Asiaticoside alleviates migraine-induced cognitive impairment via TLR4-Mediated apoptosis regulation. [Abstract]

2025 Sep 30:178204. PMID: 41038367
J Gastroenterol

Heparan sulfate acts as an activator of the NLRP3 inflammasome promoting inflammatory response in the development of acute pancreatitis. [Abstract]

2024 Sep;59(9):869-879. PMID: 38864913
Eur J Pharmacol

Direct inhibition of microglial activation by a μ receptor selective agonist alleviates inflammatory-induced pain hypersensitivity. [Abstract]

2023 Dec 15:961:176182. PMID: 37951488
Eur J Pharmacol

NAMPT mediates PDGF-induced pulmonary arterial smooth muscle cell proliferation by TLR4/NF-κB/PLK4 signaling pathway. [Abstract]

2023 Dec 15:961:176151. PMID: 37914064
Respir Res

MUC1 attenuates neutrophilic airway inflammation in asthma by reducing NLRP3 inflammasome-mediated pyroptosis through the inhibition of the TLR4/MyD88/NF-κB pathway. [Abstract]

2023 Oct 25;24(1):255. PMID: 37880668
Eur J Pharmacol

Baicalin prevents fibrosis of human trabecular meshwork cells via inhibiting the MyD88/NF-κB pathway. [Abstract]

2023 Jan 5:938:175425. PMID: 36442621
Front Endocrinol

Toll-Like Receptor 4 Inhibits Estradiol Secretion via NF-κB Signaling in Human Granulosa Cells. [Abstract]

2021 Mar 12:12:629554. PMID: 33776924
Cell Biol Toxicol

SREBF2 triggers endoplasmic reticulum stress and Bax dysregulation to promote lipopolysaccharide-induced endothelial cell injury. [Abstract]

2022 Feb;38(1):185-201. PMID: 33677747
Int Immunopharmacol

Cauloside A interacts with TLR4 to induce JNK/Caspase-3/GSDME-dependent pyroptosis in non-small cell lung cancer cells. [Abstract]

2026 Jul 15:181:116687. PMID: 42085840
Int Immunopharmacol

Targeting keratinocyte DC-SIGN with heparin analogue octaparin restores barrier and immune homeostasis in atopic dermatitis. [Abstract]

2026 Jul 1:180:116723. PMID: 42035549
Cell Oncol (Dordr)

P2RY6+ tumor-associated macrophages as a therapeutic target: suppressing tumor growth and enhancing chemosensitivity in triple-negative breast cancer. [Abstract]

2026 Jun 6. PMID: 42250059
Int Immunopharmacol

Repurposing Azilsartan medoxomil attenuates periodontitis by targeting SERPINB9 to promote apoptosis of IL1B+ macrophages. [Abstract]

2026 May 15:177:116523. PMID: 41864017
Int Immunopharmacol

GRK2-facilitated TLR4 signaling promotes cardiac fibrosis in rheumatic mice. [Abstract]

2025 May 7:157:114709. PMID: 40339495
Int J Mol Sci

Lidocaine Modulates Cytokine Production and Reprograms the Tumor Immune Microenvironment to Enhance Anti-Tumor Immune Responses in Gastric Cancer. [Abstract]

2025 Mar 31;26(7):3236. PMID: 40244064
Int Immunopharmacol

TAK-242 attenuates NLRP3-ASC inflammasome-mediated neuroinflammation via TLR4/NF-κB pathway in rat experimental autoimmune neuritis. [Abstract]

2025 Apr 24:153:114429. PMID: 40112603
Int Immunopharmacol

ATP citrate lyase ablation hampers exocrine regeneration via TLR4/NF-kappaB signaling after acute pancreatitis in mice. [Abstract]

2024 Oct 31;143(Pt 3):113485. PMID: 39486178
Int J Mol Sci

GSP1-111 Modulates the Microglial M1/M2 Phenotype by Inhibition of Toll-like Receptor 2: A Potential Therapeutic Strategy for Depression. [Abstract]

2024 Oct 1;25(19):10594. PMID: 39408923
Int Immunopharmacol

High-fat diet led to testicular inflammation and ferroptosis via dysbiosis of gut microbes. [Abstract]

2024 Sep 26;142(Pt B):113235. PMID: 39332089
Int Immunopharmacol

Gut microbiome-mediated monocytes promote liver metastasis. [Abstract]

2024 May 30:133:111877. PMID: 38608440
Int Immunopharmacol

Hepatocytes-derived Prdx1 regulates macrophage phenotypes via TLR4 activation in acute liver injury. [Abstract]

2024 Jan 25:127:111439. PMID: 38159556
Int Immunopharmacol

A polysaccharide from Codonopsis pilosula roots attenuates carbon tetrachloride-induced liver fibrosis via modulation of TLR4/NF-κB and TGF-β1/Smad3 signaling pathway. [Abstract]

2023 Jun:119:110180. PMID: 37068337
Int Immunopharmacol

Escherichia coli enhances Th17/Treg imbalance via TLR4/NF-κB signaling pathway in oral lichen planus. [Abstract]

2023 Jun:119:110175. PMID: 37058754
Int Immunopharmacol

Phenylacetylglutamine increases the susceptibility of ventricular arrhythmias in heart failure mice by exacerbated activation of the TLR4/AKT/mTOR signaling pathway. [Abstract]

2023 Mar:116:109795. PMID: 36736224
Int J Mol Sci

Characteristics of an In Vitro Mesenteric Lymph Node Cell Suspension Model and Its Possible Association with In Vivo Functional Evaluation. [Abstract]

2022 Jan 17;23(2):1003. PMID: 35055188
Int J Mol Sci

Cordyceps militaris Immunomodulatory Protein Promotes the Phagocytic Ability of Macrophages through the TLR4-NF-κB Pathway. [Abstract]

2021 Nov 11;22(22):12188. PMID: 34830071
Int Immunopharmacol

TLR4/TRAF6/NOX2 signaling pathway is involved in ventilation-induced lung injury via endoplasmic reticulum stress in murine model. [Abstract]

2021 Jul:96:107774. PMID: 34020396
Int J Mol Sci

A Combined Activity of Thrombin and P-Selectin Is Essential for Platelet Activation by Pancreatic Cancer Cells. [Abstract]

2021 Mar 24;22(7):3323. PMID: 33805059
Zool Res

Dmrt1 regulates the immune response by repressing the TLR4 signaling pathway in goat male germline stem cells. [Abstract]

2021 Jan 18;42(1):14-27. PMID: 33420764
Int Immunopharmacol

Pretreatment with resveratrol ameliorate trigeminal neuralgia by suppressing matrix metalloproteinase-9/2 in trigeminal ganglion. [Abstract]

2019 Jul:72:339-347. PMID: 31009895
Int Immunopharmacol

LPS induces CXCL16 expression in HUVECs through the miR-146a-mediated TLR4 pathway. [Abstract]

2019 Apr:69:143-149. PMID: 30710793
Int Immunopharmacol

Protective effects of ginsenoside Rg1 against lipopolysaccharide/d-galactosamine-induced acute liver injury in mice through inhibiting toll-like receptor 4 signaling pathway. [Abstract]

2018 Aug:61:266-276. PMID: 29902710

Resatorvid purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2018 Aug:61:266-276. [Abstract]

The protein expressions of TLR4 and NF-κB p65 are measured by western blot.
Mol Neurobiol

Effect of Early Inhibition of Toll-Like Receptor 4 on Hippocampal Plasticity in a Neonatal Rat Model of Hypoxic-Ischemic Brain Damage. [Abstract]

2025 Jan;62(1):1067-1078. PMID: 38954251
Neurochem Int

Downregulation of Nogo-B ameliorates cerebral ischemia/reperfusion injury in mice through regulating microglia polarization via TLR4/NF-kappaB pathway. [Abstract]

2023 Jul:167:105553. PMID: 37230196
Front Cell Infect Microbiol

Lipopolysaccharide Preparation Derived From Porphyromonas gingivalis Induces a Weaker Immuno-Inflammatory Response in BV-2 Microglial Cells Than Escherichia coli by Differentially Activating TLR2/4-Mediated NF-κB/STAT3 Signaling Pathways. [Abstract]

2021 Mar 18:11:606986. PMID: 33816329
Neurochem Int

TLR4-mediated hippocampal MMP/TIMP imbalance contributes to the aggravation of perioperative neurocognitive disorder in db/db mice. [Abstract]

2020 Nov;140:104818. PMID: 32758588
Arthritis Res Ther

Bone marrow mesenchymal stem cell-derived exosomes improve pyroptosis and mitochondrial integrity through miR-515-5p-mediated TLR4/NLRP3/GSDMD axis in rheumatoid arthritis. [Abstract]

2025 Dec 15;27(1):226. PMID: 41398286
J Clin Endocrinol Metab

Gram-negative bacteria and lipopolysaccharides as risk factors for the occurrence of diabetic foot. [Abstract]

2023 Sep 18;108(10):2604-2614. PMID: 36974462
Am J Respir Cell Mol Biol

Neuromedin U Induces Pulmonary ILC2 Activation via the NMUR1 Pathway During Acute RSV Infection. [Abstract]

2023 Mar;68(3):256-266. PMID: 36227802
Front Pharmacol

Strongylocentrotus nudus Eggs Polysaccharide Enhances Macrophage Phagocytosis Against E.coli Infection by TLR4/STAT3 Axis. [Abstract]

2022 Mar 17;13:807440. PMID: 35370674
Front Pharmacol

A Polysaccharide From Eupolyphaga sinensis Walker With Anti-HBV Activities In Vitro and In Vivo. [Abstract]

2022 Mar 3;13:827128. PMID: 35308231
Immunology

Adipose invariant NKT cells interact with CD1d-expressing macrophages to regulate obesity-related inflammation. [Abstract]

2022 Apr;165(4):414-427. PMID: 35137411
Front Pharmacol

Recombinant Ricin Toxin Binding Subunit B (RTB) Stimulates Production of TNF-α by Mouse Macrophages Through Activation of TLR4 Signaling Pathway. [Abstract]

2020 Sep 8;11:526129. PMID: 33013378
Front Pharmacol

Bacteroides Fragilis Polysaccharide A Ameliorates Abnormal Voriconazole Metabolism Accompanied With the Inhibition of TLR4/NF-κB Pathway. [Abstract]

2021 Apr 15:12:663325. PMID: 33995087
Front Pharmacol

Polysaccharide Isolated From Tetrastigma hemsleyanum Activates TLR4 in Macrophage Cell Lines and Enhances Immune Responses in OVA-Immunized and LLC-Bearing Mouse Models. [Abstract]

2021 Mar 24:12:609059. PMID: 33841142
Inflammation

Toll-like Receptor 4 Inhibitor TAK-242 Improves Fulminant Hepatitis by Regulating Accumulation of Myeloid-Derived Suppressor Cell. [Abstract]

2021 Apr;44(2):671-681. PMID: 33083887
Front Pharmacol

Asiaticoside Attenuates Cell Growth Inhibition and Apoptosis Induced by Aβ1-42 via Inhibiting the TLR4/NF-κB Signaling Pathway in Human Brain Microvascular Endothelial Cells. [Abstract]

2018 Jan 30:9:28. PMID: 29441018

Resatorvid purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 30:9:28. [Abstract]

Effects of TAK-242 on the protein expressions of TLR4, MyD88, TRAF6, p-NF-κB p65, and total NF-κB p65 induced by Aβ_1-42 in hBMECs by Western blotting analysis. The bands of TLR4, MyD88, TRAF6, p-NF-κB p65, total NF-κB p65, and β-actin. β-actin is used as a loading control.
Toxicology

Sorafenib induces intestinal toxicity by disturbing gut microbiota and activating the LPS/TLR4/NF-κB signaling pathway in mice. [Abstract]

2025 Jun 13:517:154220. PMID: 40518001
J Nutr Biochem

Chronic high-fat diet induces galectin-3 and TLR4 to activate NLRP3 inflammasome in NASH. [Abstract]

2023 Feb:112:109217. PMID: 36402251
Chem Biol Interact

Harpagide alleviate neuronal apoptosis and blood-brain barrier leakage by inhibiting TLR4/MyD88/NF-κB signaling pathway in Angiotensin II-induced microglial activation in vitro. [Abstract]

2021 Oct 1:348:109653. PMID: 34516974
Chem Biol Interact

Inhibiting expression of HSP60 and TLR4 attenuates paraquat-induced microglial inflammation. [Abstract]

2019 Feb 1;299:179-185. PMID: 30584891

Resatorvid purchased from MedChemExpress. Usage Cited in: Chem Biol Interact. 2019 Feb 1;299:179-185. [Abstract]

Western blot analysis of TLR4 and MyD88 showing effect of TLR4 inhibitor (CLI-095) on PQ-induced inflammation in BV2 microglia. The blots are representative of three independent experiments. The bar diagrams which reflect mean fold change in the expression levels of TLR4 and MyD88 with respect to the control.
Tissue Eng Regen Med

Inhibition of Toll-Like Receptor 4 Signaling Pathway Accelerates the Repair of Avascular Necrosis of Femoral Epiphysis through Regulating Macrophage Polarization in Perthes Disease. [Abstract]

2023 Jun;20(3):489-501. PMID: 37041432
Molecules

The Protective Effects of Goitrin on LPS-Induced Septic Shock in C57BL/6J Mice via Caspase-11 Non-Canonical Inflammasome Inhibition. [Abstract]

2023 Mar 23;28(7):2883. PMID: 37049646
Molecules

1,4- β-d-Glucomannan from Dendrobium officinale Activates NF- к B via TLR4 to Regulate the Immune Response. [Abstract]

2018 Oct 16;23(10). pii: E2658. PMID: 30332800
Molecules

Immunomodulatory Activity of Octenyl Succinic Anhydride Modified Porang (Amorphophallus oncophyllus) Glucomannan on Mouse Macrophage-Like J774.1 Cells and Mouse Primary Peritoneal Macrophages. [Abstract]

2017 Jul 15;22(7). pii: E1187. PMID: 28714872
Mol Med Rep

MCPIP1 alleviates depressive‑like behaviors in mice by inhibiting the TLR4/TRAF6/NF‑κB pathway to suppress neuroinflammation. [Abstract]

2024 Jan;29(1):6. PMID: 37975259
Mol Med Rep

Dexmedetomidine alleviates airway hyperresponsiveness and allergic airway inflammation through the TLR4/NF‑κB signaling pathway in mice. [Abstract]

2022 Mar;25(3):74. PMID: 35014685
Food Sci Nutr

Ovotransferrin exerts bidirectional immunomodulatory activities via TLR4-mediated signal transduction pathways in RAW264.7 cells. [Abstract]

2021 Sep 8;9(11):6162-6175. PMID: 34760247
Mol Med Rep

Serum‑derived exosomes from house dust mite‑sensitized guinea pigs contribute to inflammation in BEAS‑2B cells via the TLR4‑NF‑κB pathway. [Abstract]

2021 Nov;24(5):747. PMID: 34458929
Mol Med Rep

7‑Difluoromethyl‑5,4'‑dimethoxygenistein exerts anti‑angiogenic effects on acute promyelocytic leukemia HL‑60 cells by inhibiting the TLR4/NF‑κB signaling pathway. [Abstract]

2020 May;21(5):2251-2259. PMID: 32186776
Mol Med Rep

LPS enhances TLR4 expression and IFN‑γ production via the TLR4/IRAK/NF‑κB signaling pathway in rat pulmonary arterial smooth muscle cells. [Abstract]

2017 Sep;16(3):3111-3116. PMID: 28714001

Resatorvid purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3111-3116. [Abstract]

TLR4 inhibitor TAK 242 suppresses the TLR4/IRAK/NF ΚB signaling pathway in PASMCs. Western blot analysis is performed to detect the levels of p IRAK, IRAK, p IKK, IKK, p IκB, IκB and NF κB p65, and the representative blot results are shown.
PLoS Pathog

Retinol binding protein 4 enhances cellular cholesterol uptake to facilitate influenza A virus infection. [Abstract]

2025 Oct 27;21(10):e1013623. PMID: 41144502
Mediators Inflamm

HMGB1 Exacerbates Intestinal Barrier Damage by Inducing Ferroptosis Through the TLR4/NF-κB/GPX4 Pathway in Ulcerative Colitis. [Abstract]

2025 Jul 11:2025:2395557. PMID: 40689397
Sci Rep

GLUT1-mediated HMGB1 O-GlcNAcylation drives hyperglycemia-Induced neutrophil extracellular trap networks formation via TLR4 signaling and exacerbates fibroblast inflammation. [Abstract]

2025 May 29;15(1):18853. PMID: 40442314
Am J Pathol

Lipopolysaccharide Triggers Luminal Acidification to Promote Defense Against Bacterial Infection in Vaginal Epithelium. [Abstract]

2024 Aug 31:S0002-9440(24)00328-6. PMID: 39222908
Sci Rep

A comparative study of spike protein of SARS-CoV-2 and its variant Omicron (B.1.1.529) on some immune characteristics. [Abstract]

2022 Oct 12;12(1):17058. PMID: 36224298
Mediators Inflamm

MFG-E8 Knockout Aggravated Nonalcoholic Steatohepatitis by Promoting the Activation of TLR4/NF- κ B Signaling in Mice. [Abstract]

2022 Jun 20:2022:5791915. PMID: 35769208
Mediators Inflamm

Extracellular HMGB1 Induced Glomerular Endothelial Cell Injury via TLR4/MyD88 Signaling Pathway in Lupus Nephritis. [Abstract]

2021 Dec 21:2021:9993971. PMID: 34970076
Sci Rep

Astaxanthin protects against early acute kidney injury in severely burned rats by inactivating the TLR4/MyD88/NF-κB axis and upregulating heme oxygenase-1. [Abstract]

2021 Mar 23;11(1):6679. PMID: 33758309
Sci Rep

Honey isomaltose contributes to the induction of granulocyte-colony stimulating factor (G-CSF) secretion in the intestinal epithelial cells following honey heating. [Abstract]

2020 Sep 16;10(1):15178. PMID: 32938976
Mediators Inflamm

Biological Characterization of Commercial Recombinantly Expressed Immunomodulating Proteins Contaminated with Bacterial Products in the Year 2020: The SAA3 Case. [Abstract]

2020 Jul 6;2020:6087109. PMID: 32694927
Sci Rep

TAK-242 ameliorates contact dermatitis exacerbated by IL-36 receptor antagonist deficiency. [Abstract]

2020 Jan 20;10(1):734. PMID: 31959814
Mediators Inflamm

High-Fat Diet Aggravates the Intestinal Barrier Injury via TLR4-RIP3 Pathway in a Rat Model of Severe Acute Pancreatitis. [Abstract]

2019 Dec 17;2019:2512687. PMID: 31933540
Mediators Inflamm

Oscillatory Shear Stress Induces Oxidative Stress via TLR4 Activation in Endothelial Cells. [Abstract]

2019 Jun 17:2019:7162976. PMID: 31316302
Transplantation

Early TLR4 Blockade Attenuates Sterile Inflammation-mediated Stress in Islets During Isolation and Promotes Successful Transplant Outcomes. [Abstract]

2018 Sep;102(9):1505-1513. PMID: 29787520

Resatorvid purchased from MedChemExpress. Usage Cited in: Transplantation. 2018 Sep;102(9):1505-1513. [Abstract]

Whole-islet lysates are prepared from islets with (TAK) or without (CTRL) early TLR4 blockade immediately after isolation (0 hours) and at 6- and 24-hours postisolation. Lysates are immunoblotted for ERK1/2, P38, SAPK, and P65, and analyzed for relative activation (phospho:total) normalized to β-actin.
Cancer Sci

Resistin facilitates metastasis of lung adenocarcinoma through the TLR4/Src/EGFR/PI3K/NF-κB pathway. [Abstract]

2018 Aug;109(8):2391-2400. PMID: 29927028

Resatorvid purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Aug;109(8):2391-2400. [Abstract]

A549 cells pretreated with or without 5 μM TAK-242 and/or 10 μM PP1 (Src inhibitor) for 1 h are treated with 50 ng/mL Resistin for 15 min. Total protein is isolated and expression of phosphorylated (p-)Src, Src, p-EGFR, and EGFR is detected by Western blot
Sci Rep

9c11tCLA modulates 11t18:1 and 9t18:1 induced inflammations differently in human umbilical vein endothelial cells. [Abstract]

2018 Jan 24;8(1):1535. PMID: 29367652

Resatorvid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Jan 24;8(1):1535. [Abstract]

Effect of TAK242 on MAPKs phosphorylation in HUVECs treated with 9t18:1 and 11t18:1. HUVECs are treated with TAK242 (0.5, 1, 1.5 μM) for 30 min and then cultured with 9t18:1 for 24 h.
Sci Rep

Effects of the TLR4 signaling pathway on apoptosis of neuronal cells in diabetes mellitus complicated with cerebral infarction in a rat model. [Abstract]

2017 Mar 8;7:43834. PMID: 28272417

Resatorvid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 8;7:43834. [Abstract]

Compared with the expression in the DM + MCAO group, the expression of Bcl-2, Bax, cleaved caspase-3, TNF-α, IL-1β and TLR4 proteins is greatly reduced in the DM + MCAO + TAK242 group.
Sci Rep

Glycyrrhiza uralensis water extract enhances dendritic cell maturation and antitumor efficacy of HPV dendritic cell-based vaccine. [Abstract]

2017 Mar 8;7:43796. PMID: 28272545
Sci Rep

Soluble egg antigens of Schistosoma japonicum induce senescence in activated hepatic stellate cells by activation of the STAT3/p53/p21 pathway. [Abstract]

2016 Aug 4;6:30957. PMID: 27489164

Resatorvid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Aug 4;6:30957. [Abstract]

SEA promotes the senescence of LX-2 cells through activation of TLR4 signaling. Western blot analysis for P-p53 or TLR4 in LX-2 cells treated with SEA or TLR4 inhibitor TAK-242 (1 nM).
Sci Rep

Oxidized Low-Density Lipoprotein Induces Apoptosis in Cultured Neonatal Rat Cardiomyocytes by Modulating the TLR4/NF-κB Pathway. [Abstract]

2016 Jun 9;6:27866. PMID: 27279424

Resatorvid purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Jun 9;6:27866. [Abstract]

Examination of TLR4 expression level in each group. The protein and mRNA levels of TLR4 are down-regulated by pretreatment with TAK-242.
Sci Rep

Cellular uptake of exogenous calcineurin B is dependent on TLR4/MD2/CD14 complexes, and CnB is an endogenous ligand of TLR4. [Abstract]

2016 Apr 19;6:24346. PMID: 27090571
Pestic Biochem Physiol

Dietary supplementation of Lactobacillus casei alleviates permethrin exposure-induced zebrafish testis damage through modulation of TLR4/NF-κB and AKT/Nrf2 pathways: Oxidative stress, inflammation and ferroptosis. [Abstract]

2025 Aug:212:106450. PMID: 40500058
Exp Neurol

Role of TREM-1 in the development of early brain injury after subarachnoid hemorrhage. [Abstract]

2021 Jul:341:113692. PMID: 33727099
Cell Signal

Clec7a promotes hippocampal microglial activation in rats with status epilepticus via inducing the TLR4/MyD88/NF-κB signaling pathway. [Abstract]

2026 Aug:144:112553. PMID: 42025892
Neuropharmacology

TIM3 attenuates morphine antinociceptive tolerance and microglial neuroinflammation by suppressing the TRAF6/NF-κB pathway in male mice. [Abstract]

2025 Nov 15:279:110638. PMID: 40840715
J Cell Mol Med

Pan-Cancer Analyses of Necroptosis, Pyroptosis and Ferroptosis Related Genes Reveal TLR4 as A Potential Therapeutic Target. [Abstract]

2025 Jul;29(14):e70742. PMID: 40696496
Microorganisms

The Role of TLR4 in Lung Epithelial Cell Injury Caused by Influenza Virus Combined with Staphylococcus aureus. [Abstract]

2025 May 24;13(6):1201. PMID: 40572089
J Dairy Sci

Immunomodulatory effects, digestive stability, and action mechanism of casein peptide SPAQILQW in activating macrophages via N-terminal serine. [Abstract]

2025 Apr 28:S0022-0302(25)00284-X. PMID: 40306417
Cell Signal

Programmed cell death 10 increased blood-brain barrier permeability through HMGB1/TLR4 mediated downregulation of endothelial ZO-1 in glioblastoma. [Abstract]

2023 Jul:107:110683. PMID: 37075875
J Dairy Sci

Forkhead box protein A2 alleviates toll-like receptor 4-mediated inflammation, endoplasmic reticulum stress, autophagy, and apoptosis induced by lipopolysaccharide in bovine hepatocytes. [Abstract]

2023 Mar;106(3):2089-2112. PMID: 36586798
Microorganisms

Lactobacillus johnsonii L531 Alleviates the Damage Caused by Salmonella Typhimurium via Inhibiting TLR4, NF-κB, and NLRP3 Inflammasome Signaling Pathways. [Abstract]

2021 Sep 17;9(9):1983. PMID: 34576878
J Dairy Sci

Role of long polar fimbriae type 1 and 2 in pathogenesis of mammary pathogenic Escherichia coli. [Abstract]

2021 Jul;104(7):8243-8255. PMID: 33814154
J Cell Mol Med

TLR4 contributes to the damage of cartilage and subchondral bone in discectomy-induced TMJOA mice. [Abstract]

2020 Oct;24(19):11489-11499. PMID: 32914937
J Cell Mol Med

LIGHT aggravates sepsis-associated acute kidney injury via TLR4-MyD88-NF-κB pathway. [Abstract]

2020 Oct;24(20):11936-11948. PMID: 32881263
Oncol Rep

Low-dose paclitaxel suppresses the induction of M2 macrophages in gastric cancer. [Abstract]

2017 Jun;37(6):3341-3350. PMID: 28440494
J Inflamm Res

The EZH2 Inhibitor GSK126 Alleviates Thromboinflammation in Deep Vein Thrombosis by Suppressing TLR4 Signaling via H3K27me3 Modulation. [Abstract]

2025 Oct 2:18:13519-13534. PMID: 41059285
J Inflamm Res

Aqueous Extract of Cimicifuga dahurica Reprogramming Macrophage Polarization by Activating TLR4-NF-κB Signaling Pathway. [Abstract]

2022 Feb 15;15:1027-1046. PMID: 35210810
J Neurochem

Ulinastatin inhibited sepsis-induced spinal inflammation to alleviate peripheral neuromuscular dysfunction in an experimental rat model of neuromyopathy. [Abstract]

2017 Oct;143(2):225-235. PMID: 28796387
J Neurochem

Preconditioning with recombinant high-mobility group box 1 induces ischemic tolerance in a rat model of focal cerebral ischemia-reperfusion. [Abstract]

2016 May;137(4):576-88. PMID: 26991073

Resatorvid purchased from MedChemExpress. Usage Cited in: J Neurochem. 2016 May;137(4):576-88. [Abstract]

TAK-242 markedly inhibits the up-regulation of IRAK-M and the down-regulation of p-IRAK-1 in rHMGB1-pretreated rats underwent MCAO. WB analysis of IRAK-M and p-IRAK-1 in rat ipsilateral hemispheres.
iScience

IGFL2 suppresses gastric cancer cell sensitivity to docetaxel by activating the Toll-like receptor signaling pathway. [Abstract]

2026 May 29;29(6):116246. PMID: 42256293
ACS Infect Dis

Treponema pallidum Flagellin FlaB3 Activates Inflammation and Inhibits Autophagy in HMC3 Cells via the TLR4 Pathway. [Abstract]

2025 Mar 14;11(3):773-783. PMID: 40036177
Brain Res Bull

Remimazolam ameliorates postoperative cognitive dysfunction after deep hypothermic circulatory arrest through HMGB1-TLR4-NF-κB pathway. [Abstract]

2024 Oct 15:217:111086. PMID: 39322086
Mol Nutr Food Res

Profiles of Intestinal Flora in Breastfed Obese Children and Selecting Functional Strains Against Obesity. [Abstract]

2024 Feb;68(4):e2300735. PMID: 38227364
ACS Chem Neurosci

Thymoquinone Alleviates Paclitaxel-Induced Peripheral Neuropathy through Regulation of the TLR4-MyD88 Inflammatory Pathway. [Abstract]

2023 Oct 18;14(20):3804-3817. PMID: 37813830
Metabolites

Palmitic Acid Promotes Lung Metastasis of Melanomas via the TLR4/TRIF-Peli1-pNF-κB Pathway. [Abstract]

2022 Nov 17;12(11):1132. PMID: 36422271

Resatorvid purchased from MedChemExpress. Usage Cited in: Metabolites. 2022 Nov 17;12(11):1132. [Abstract]

Resatorvid (TAK-242; 0.1, 1, 10, 50 µM; 24 h) inhibits the proliferation of B16 cells and A375 cells in a dose-dependent manner.
Biomed Environ Sci

Effects of Combination of 1,25(OH) 2D 3 and TLR-4 Inhibitor on the Damage to HaCaT Cells Caused by UVB Irradiation. [Abstract]

022 Nov 20;35(11):1051-1062. PMID: 36443257
J Periodontol

The role of PHF8 and TLR4 in osteogenic differentiation of periodontal ligament cells in inflammatory environment. [Abstract]

2021 Jul;92(7):1049-1059. PMID: 33040333
Brain Res Bull

TLR4 inhibition ameliorates mesencephalic substantia nigra injury in neonatal rats exposed to lipopolysaccharide via regulation of neuro-immunity. [Abstract]

2020 Dec;165:90-96. PMID: 32956769
Neurochem Res

Interleukin-1 Receptor Associated Kinase 1 Mediates the Maintenance of Neuropathic Pain after Chronic Constriction Injury in Rats. [Abstract]

2019 May;44(5):1214-1227. PMID: 30859436
FASEB J

Dual Pro-Angiogenic and Pro-Fibrotic MARCO+ Microglial Phenotype in Diabetic Retinopathy. [Abstract]

2025 Sep 15;39(17):e71006. PMID: 40888751
FASEB J

Toll-like receptor 4-dependent innate immune responses are mediated by intracrine corticosteroids and activation of glycogen synthase kinase-3β in astrocytes. [Abstract]

2024 Jul 15;38(13):e23781. PMID: 38941212
FASEB J

The ecotin-like peptidase inhibitor of Trypanosoma cruzi prevents TMPRSS2-PAR2-TLR4 crosstalk downmodulating infection and inflammation. [Abstract]

2024 Mar 31;38(6):e23566. PMID: 38526868
FASEB J

Serum amyloid A aggravates endotoxin-induced ocular inflammation through the regulation of retinal microglial activation. [Abstract]

2024 Jan;38(1):e23389. PMID: 38153347
Antiviral Res

Human adenovirus type 7 virus-like particle vaccine induces Dendritic cell maturation through the TLR4/NF-κB pathway and is highly immunogenic. [Abstract]

2023 Feb 20;105559. PMID: 36813181
Biol Trace Elem Res

Selenium Deficiency Induces Autophagy in Chicken Bursa of Fabricius Through ChTLR4/MyD88/NF-κB Pathway. [Abstract]

2022 Jul;200(7):3303-3314. PMID: 34467441
J Neurosci

Temporal Contribution of Myeloid-Lineage TLR4 to the Transition to Chronic Pain: A Focus on Sex Differences. [Abstract]

2021 May 12;41(19):4349-4365. PMID: 33846230
Front Physiol

Chronic Unpredictable Mild Stress Promotes Atherosclerosis via HMGB1/TLR4-Mediated Downregulation of PPARγ/LXRα/ABCA1 in ApoE-/- Mice. [Abstract]

2019 Mar 1:10:165. PMID: 30881312

Resatorvid purchased from MedChemExpress. Usage Cited in: Front Physiol. 2019 Mar 1:10:165. [Abstract]

Effect of EP and TAK-242 treatment on CD68 protein expressions in aortic sinus of CUMS ApoE^-/- mice. Over a 16-week period treatment, entire aorta from the aortic root to the iliac bifurcation is harvested, and then frozen-sections of aortic sinus are performed for immunofluorescent staining of CD68. Representative images of CD68 expression in aortic sinus.
FASEB J

Role of TLR4-MAP4K4 signaling pathway in models of oxygen-induced retinopathy. [Abstract]

2019 Mar;33(3):3451-3464. PMID: 30475644

Resatorvid purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Mar;33(3):3451-3464. [Abstract]

Western blot analyses of TLR4 and MAP4K4 in the retina of PN 17 OIR mice with or without TAK-242 treatment.

Resatorvid purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Mar;33(3):3451-3464. [Abstract]

Western blot analyses of TLR4 and MAP4K4, and moesin phosphorylation in HRMECs with the different treatments of TAK-242 or LPS.
Prog Neuropsychopharmacol Biol Psychiatry

Microglial NLRP3 inflammasome activation mediates diabetes-induced depression-like behavior via triggering neuroinflammation. [Abstract]

2023 Aug 30:126:110796. PMID: 37209992
Korean J Pain

Toll-like receptor 4/nuclear factor-kappa B pathway is involved in radicular pain by encouraging spinal microglia activation and inflammatory response in a rat model of lumbar disc herniation. [Abstract]

2021 Jan 1;34(1):47-57. PMID: 33380567
Mol Hum Reprod

Excess palmitate induces decidual stromal cell apoptosis via the TLR4/JNK/NF-kB pathways and possibly through glutamine oxidation. [Abstract]

2020 Feb 29;26(2):88-100. PMID: 31977025
Am J Physiol Endocrinol Metab

C/EBPβ mediates palmitate-induced musclin expression via the regulation of PERK/ATF4 pathways in myotubes. [Abstract]

2019 Jun 1;316(6):E1081-E1092. PMID: 30964708
J Clin Immunol

S100A4 Induces Neutrophilic Inflammation in Chronic Rhinosinusitis with Nasal Polyps via TLR4 Pathway. [Abstract]

2025 Nov 15;45(1):160. PMID: 41240201
J Food Sci

Galacturonic Acid Alleviates Lipopolysaccharide-Induced Macrophage Inflammation Potentially Through Competitively Inhibiting the TLR4/NF-κB Pathway. [Abstract]

2025 Oct;90(10):e70622. PMID: 41090497
Mycopathologia

MiR-146a Negatively Regulates Aspergillus fumigatus-Induced TNF-α and IL-6 Secretion in THP-1 Macrophages. [Abstract]

2021 Jun;186(3):341-354. PMID: 34089172
J Biol Chem

Signaling between pancreatic β cells and macrophages via S100 calcium-binding protein A8 exacerbates β-cell apoptosis and islet inflammation. [Abstract]

2018 Apr 20;293(16):5934-5946. PMID: 29496993
J Immunol

TLR4al senses heme as a key damage/danger-associated molecular pattern to activate immune responses in lower vertebrates. [Abstract]

2025 Aug 19:vkaf192. PMID: 40829171
J Immunol

HMGB1 inhibits the IFN-γ-induced PD-L1 expression in NSCLC. [Abstract]

2025 Jun 28:vkaf125. PMID: 40580518
Front Neurosci

S100A8 Promotes Inflammation via Toll-Like Receptor 4 After Experimental Traumatic Brain Injury. [Abstract]

2021 Feb 3:14:616559. PMID: 33613176
J Immunol

Proinflammatory S100A8 Induces PD-L1 Expression in Macrophages, Mediating Tumor Immune Escape. [Abstract]

2020 May 1;204(9):2589-2599. PMID: 32198140
J Cell Physiol

Gestational diabetes mellitus affects odontoblastic differentiation of dental papilla cells via Toll-like receptor 4 signaling in offspring. [Abstract]

2020 Apr;235(4):3519-3528. PMID: 31595494
J Cell Physiol

Follistatin-like protein 1 induction of matrix metalloproteinase 1, 3 and 13 gene expression in rheumatoid arthritis synoviocytes requires MAPK, JAK/STAT3 and NF-κB pathways. [Abstract]

2018 Jan;234(1):454-463. PMID: 29932210
J Sci Food Agric

Immunostimulatory effect of aqueous extract of Coriandrum sativum L. seed on macrophages. [Abstract]

2017 Nov;97(14):4727-4736. PMID: 28369918
Vet Q

An underlying mechanism of bovine mastitis: PGE2 regulates Staphylococcus aureus-induced inflammatory response through TLR2, TLR4, and NLRP3 in macrophages. [Abstract]

2026 Dec;46(1):2615759. PMID: 41546499
J Funct Foods

2023 Mar.
Microb Pathog

Involvement of glycoinositolphospholipid from Trypanosoma cruzi and macrophage migration inhibitory factor in proinflammatory mechanisms promoting cardiovascular injury mechanisms promoting cardiovascular inflammation tThe combined action of glycoinositolphospholipid from Trypanosoma cruzi and macrophage migration inhibitory factor increases proinflammatory mediator production by cardiomyocytes and vascular endothelial cells. [Abstract]

2022 Dec;173(Pt A):105881. PMID: 36379373
J Funct Foods

August 2022, 105166.
J Funct Foods

2020 Jun.
Pathogens

Extracellular Lipopolysaccharide Triggers the Release of Unconjugated Interferon-Stimulated Gene 15 (ISG15) Protein from Macrophages via Type-I Interferon/Caspase-4/Gasdermin-D Pathway. [Abstract]

2026 Jan 22;15(1):122. PMID: 41599106
Neurotoxicology

Thymoquinone regulates microglial M1/M2 polarization after cerebral ischemia-reperfusion injury via the TLR4 signaling pathway. [Abstract]

2024 Mar:101:54-67. PMID: 38325603
BMC Oral Health

Different expression patterns of inflammatory cytokines induced by lipopolysaccharides from Escherichia coli or Porphyromonas gingivalis in human dental pulp stem cells. [Abstract]

2022 Apr 12;22(1):121. PMID: 35413908
Viruses

Inhibiting ACSL1-Related Ferroptosis Restrains Murine Coronavirus Infection. [Abstract]

2021 Nov 28;13(12):2383. PMID: 34960652
Exp Biol Med

Nicorandil inhibits TLR4/MyD88/NF-κB/NLRP3 signaling pathway to reduce pyroptosis in rats with myocardial infarction. [Abstract]

2021 Sep;246(17):1938-1947. PMID: 34034564
Biochim Biophys Acta Mol Cell Biol Lipids

Macrophage iron retention aggravates atherosclerosis: Evidence for the role of autocrine formation of hepcidin in plaque macrophages. [Abstract]

2020 Feb;1865(2):158531. PMID: 31666189
Mol Pain

Toll like receptor (TLR)-4 as a regulator of peripheral endogenous opioid-mediated analgesia in inflammation. [Abstract]

2014 Feb 6;10(1):10. PMID: 24499354
J Bioenerg Biomembr

Intestinal microecology regulates neutrophil recruitment through TLR4/MAPK/CXCR2 signaling pathway to promote liver ischemia/reperfusion injury. [Abstract]

2026 Jun 13;58(1):32. PMID: 42287485
Food Agric Immunol

2025 Feb 08.
Mol Immunol

Activation of TLR4 induces severe acute pancreatitis-associated spleen injury via ROS-disrupted mitophagy pathway. [Abstract]

2022 Feb:142:63-75. PMID: 34965485
Int J Med Sci

Early Toll-like receptor 4 inhibition improves immune dysfunction in the hippocampus after hypoxic-ischemic brain damage. [Abstract]

2022 Jan 1;19(1):142-151. PMID: 34975308
Parasit Vectors

Involvement of TLR4 signaling regulated-COX2/PGE2 axis in liver fibrosis induced by Schistosoma japonicum infection. [Abstract]

2021 May 25;14(1):279. PMID: 34034779
Parasit Vectors

Contribution of tissue transglutaminase to the severity of hepatic fibrosis resulting from Schistosoma japonicum infection through the regulation of IL-33/ST2 expression. [Abstract]

2019 Jun 14;12(1):302. PMID: 31200771
Mol Immunol

Dehydroepiandrosterone attenuates LPS-induced inflammatory responses via activation of Nrf2 in RAW264.7 macrophages. [Abstract]

2021 Mar:131:97-111. PMID: 33461765
Mol Immunol

Asiaticoside ameliorates acinar cell necrosis in acute pancreatitis via toll-like receptor 4 pathway. [Abstract]

2021 Feb:130:122-132. PMID: 33308902
Food Agr Immunol

2020 Apr.
Vascul Pharmacol

HMGB1/TLR4 promotes hypoxic pulmonary hypertension via suppressing BMPR2 signaling. [Abstract]

2019 Jun:117:35-44. PMID: 30610955
Cytokine

Morphine induces inflammatory responses via both TLR4 and cGAS-STING signaling pathways. [Abstract]

2024 Aug 31:183:156737. PMID: 39217915
J Psychiatr Res

PAG neuronal NMDARs activation mediated morphine-induced hyperalgesia by HMGB1-TLR4 dependent microglial inflammation. [Abstract]

2023 Aug:164:150-161. PMID: 37352811
Clin Oral Investig

Lipopolysaccharide inhibits osteogenic differentiation of periodontal ligament stem cells partially through toll-like receptor 4-mediated ephrinB2 downregulation. [Abstract]

2020 Oct;24(10):3407-3416. PMID: 31974644
Am J Physiol Renal Physiol

Cystitis-induced bladder pain is Toll-like receptor 4 dependent in a transgenic autoimmune cystitis murine model: a MAPP Research Network animal study. [Abstract]

2019 Jul 1;317(1):F90-F98. PMID: 31091120
J Radiat Res Appl Sci

2026 Mar 13.
Exp Cell Res

HMGB1 contributes to pancreatic fibrosis by regulating TLR4-mediated autophagy and the NLRP3 inflammasome pathway in chronic pancreatitis. [Abstract]

2025 Sep 1;452(1):114745. PMID: 40915340
Exp Cell Res

Mechanism of pro-MMP9 activation in co-culture of pro-inflammatory macrophages and cardiomyocytes. [Abstract]

2024 Jan 1;434(1):113868. PMID: 38043722
Immun Inflamm Dis

Activation of Toll-like receptor 4 by thyroid hormone triggers abnormal B-cell activation. [Abstract]

2023 Sep;11(9):e1007. PMID: 37773690
Arch Biochem Biophys

Gasdermin D is involved in switching from apoptosis to pyroptosis in TLR4-mediated renal tubular epithelial cells injury in diabetic kidney disease. [Abstract]

2022 Sep 30:727:109347. PMID: 35809639
Cancer Med

The immunostimulatory effects and pro-apoptotic activity of rhCNB against Lewis lung cancer is mediated by Toll-like receptor 4. [Abstract]

2019 Aug;8(9):4441-4453. PMID: 31218844
Exp Cell Res

Macrophages enhance tumor-derived autophagosomes (DRibbles)-induced B cells activation by TLR4/MyD88 and CD40/CD40L. [Abstract]

2015 Feb 15;331(2):320-30. PMID: 25447440
J Atheroscler Thromb

2026 Feb.
Infect Immun

Toll-Like Receptor 2 (TLR2) and TLR4 Mediate the IgA Immune Response Induced by Mycoplasma hyopneumoniae. [Abstract]

2019 Dec 17;88(1):e00697-19. PMID: 31611272
Cancer Prev Res (Phila)

Pharmacological TLR4 Antagonism Using Topical Resatorvid Blocks Solar UV-Induced Skin Tumorigenesis in SKH-1 Mice. [Abstract]

2018 May;11(5):265-278. PMID: 29437671

Resatorvid purchased from MedChemExpress. Usage Cited in: Cancer Prev Res (Phila). 2018 May;11(5):265-278. [Abstract]

There is a remarkable reduction in average levels of p21^waf1 expression in the Prevention tumors compared to controls.
Vaccine

Adjuvant-active aqueous extracts from Artemisia rupestris L. improve immune responses through TLR4 signaling pathway. [Abstract]

2017 Feb 15;35(7):1037-1045. PMID: 28111143
Vaccine

Pleurotus ferulae water extract enhances the maturation and function of murine bone marrow-derived dendritic cells through TLR4 signaling pathway. [Abstract]

2015 Apr 15;33(16):1923-33. PMID: 25748337
Cell Immunol

House dust mite allergen directly activates ILC2 cells via the TLR4 signaling pathway in allergic airway diseases. [Abstract]

2024 Nov-Dec:405-406:104884. PMID: 39437527
J Neuropathol Exp Neurol

Sevoflurane anesthesia during late gestation induces cognitive disorder in rat offspring via the TLR4/BDNF/TrkB/CREB pathway. [Abstract]

2024 Sep 13:nlae096. PMID: 39271176
Cell Immunol

LPS enhances platelets aggregation via TLR4, which is related to mitochondria damage caused by intracellular ROS, but not extracellular ROS. [Abstract]

2018 Jun:328:86-92. PMID: 29653689

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Immunol. 2018 Jun:328:86-92. [Abstract]

Washed platelets are dealt with LPS (10 ug/mL, 30 min), LPS (10 ug/mL, 30 min) and TAK242 (132 nM, 30 min) or vehicle. PKC, AKT and p38 are detected by western blotting.
Neuroscience

HMGB1 binding heptamer peptide improves survival and ameliorates brain injury in rats after cardiac arrest and cardiopulmonary resuscitation. [Abstract]

2017 Sep 30:360:128-138. PMID: 28778700
Biochem Biophys Rep

Quantitative analysis of hemin-induced neutrophil extracellular trap formation and effects of hydrogen peroxide on this phenomenon. [Abstract]

2017 Jul 24:11:147-153. PMID: 28955779
Adv Biol (Weinh)

HMGB1 Derived from the Pyroptotic Microenvironment Promotes Macrophage Extracellular Traps in Hirschsprung-Associated Enterocolitis. [Abstract]

2025 Jun 4:e00761. PMID: 40464207

Resatorvid purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]

The MET formation of macrophages pretreated with inhibitors of TLR2 (HY‐112146; MMG-11), TLR4 (HY‐11109; Resatorvid) and RAGE (HY‐P2268; RAGE antagonist peptide) prior to incubation with pyroptotic‐CM was evaluated with SYTOX Green staining and detected by flow cytometry.

Resatorvid purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]

Macrophages were pretreated with inhibitors of TLR2 (MMG-11; HY‐112146), TLR4 (Resatorvid; HY‐11109), TLR9 (TLR7/8/9-IN-1; HY-131952) and RAGE (RAGE antagonist peptide; HY‐P2268) prior to coculture with pyroptotic‐CM, and the p‐p38 and p‐p65 levels in macrophages were measured by western blotting.

Resatorvid purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]

The MET formation of macrophages pretreated with inhibitors of (MMG-11; HY‐112146), TLR4 (Resatorvid; HY‐11109) and RAGE (RAGE antagonist peptide; HY‐P2268) prior to incubation with pyroptotic‐CM was detected by flow cytometry.
Brain Res

Galectin-3 activates microglia and promotes neurological impairment via NLRP3/pyroptosis pathway following traumatic brain injury. [Abstract]

2025 May 15:1855:149560. PMID: 40074166
Adv Ther (Weinh)

2024 Sep 09.
Food Chem Toxicol

The role of HMGB1 on SiC NPs-induced inflammation response in lung epithelial-macrophage co-culture system. [Abstract]

2024 Jun 11:190:114762. PMID: 38871110
Immunol Lett

Neonatal Streptococcus Pneumoniae pneumonia induces airway SMMHC expression through HMGB1/TLR4/ERK. [Abstract]

2021 Dec:240:149-158. PMID: 34732321
Curr Pharm Des

Interaction of Ectodomain of Respiratory Syncytial Virus G Protein with TLR2/ TLR6 Heterodimer: An In vitro and In silico Approach to Decipher the Role of RSV G Protein in Pro-inflammatory Response against the Virus. [Abstract]

2021;27(44):4464-4476. PMID: 34279194
J Immunol Res

Lycium barbarum Polysaccharides Promote Maturity of Murine Dendritic Cells through Toll-Like Receptor 4-Erk1/2-Blimp1 Signaling Pathway. [Abstract]

2020 Dec 1;2020:1751793. PMID: 33344654
J Immunol Res

Prevotella Induces the Production of Th17 Cells in the Colon of Mice. [Abstract]

2020 Nov 1;2020:9607328. PMID: 33204736
J Neurosci Res

PPP1R15A Promotes Apoptosis, Autophagy, and Inflammatory Response to Exacerbate Ischemic Stroke Through Activation of TLR4/NF-κB Pathway. [Abstract]

2025 Aug;103(8):e70073. PMID: 40751334
Exp Eye Res

TLR4 signal inhibition alleviates alkali-burn induced corneal neovascularization. [Abstract]

2025 Sep:258:110486. PMID: 40527362
Chin J Integr Med

Electroacupuncture Attenuates Immune-Inflammatory Response in Hippocampus of Rats with Vascular Dementia by Inhibiting TLR4/MyD88 Signaling Pathway. [Abstract]

2022 Feb;28(2):153-161. PMID: 34913150
Exp Eye Res

N-acetylserotonin alleviated the expression of interleukin-1β in retinal ischemia-reperfusion rats via the TLR4/NF-κB/NLRP3 pathway. [Abstract]

2021 Jul:208:108595. PMID: 34000276
J Neuroimmunol

Protective effect of scorpion venom heat-resistant synthetic peptide against PM2.5-induced microglial polarization via TLR4-mediated autophagy activating PI3K/AKT/NF-κB signaling pathway. [Abstract]

2021 Jun 15:355:577567. PMID: 33887539
Am J Cancer Res

FSTL1 promotes growth and metastasis in gastric cancer by activating AKT related pathway and predicts poor survival. [Abstract]

2021 Mar 1;11(3):712-728. PMID: 33791149
J Neurol Sci

Attenuation of paraquat-induced inflammation by inhibitors of phosphorylation of mitogen-activated protein kinases in BV2 microglial cells. [Abstract]

2020 Mar 15;410:116679. PMID: 31951835
Toxicol Lett

Perinatal exposure to nonylphenol induces microglia-mediated nitric oxide and prostaglandin E2 production in offspring hippocampus. [Abstract]

2019 Feb:301:114-124. PMID: 30481583
Global Spine J

2018 May; 8(1 Suppl): 174S-374S.
Haemophilia

Inhibition of CIRBP as a Novel Strategy to Alleviate Chondrocyte Ferroptosis in Haemophilic Arthropathy. [Abstract]

2025 Dec 22. PMID: 41427808
J Cell Biochem

Effect of oleic acid on induction of steatosis and cytotoxicity in BRL 3A cells. [Abstract]

2019 Dec;120(12):19541-19554. PMID: 31264285
Am J Physiol Gastrointest Liver Physiol

Catalpol restores LPS-elicited rat microcirculation disorder by regulation of a network of signaling involving inhibition of TLR-4 and SRC. [Abstract]

2016 Dec 1;311(6):G1091-G1104. PMID: 27789455

Resatorvid purchased from MedChemExpress. Usage Cited in: Am J Physiol Gastrointest Liver Physiol. 2016 Dec 1;311(6):G1091-G1104. [Abstract]

Effects of TAK 242 and Catalpol on the expression of TLR-4 and activation of Src, PI3K, FAK, and Cathepsin B induced by LPS in HUVECs. Representative Western blots of TLR-4, p-Src, Src, p-PI3K, PI3K, p-FAK, FAK, activated cathepsin B, and cathepsin B proenzyme in different groups.
Am J Physiol Gastrointest Liver Physiol

Inhibition of Toll-like receptor 4 suppresses liver injury induced by biliary obstruction and subsequent intraportal lipopolysaccharide injection. [Abstract]

2014 Feb;306(3):G244-52. PMID: 24356883
Fitoterapia

The processed Euphorbia lathyris L. alleviates the inflammatory injury via regulating LXRα/ABCA1 expression and TLR4 positioning to lipid rafts. [Abstract]

2024 Jul 4:106111. PMID: 38971330
Theriogenology

Downregulation of XBP1s aggravates lipopolysaccharide-induced inflammation by promoting NF-κB and NLRP3 pathways' activation in goat endometrial epithelial cells. [Abstract]

2023 Oct 15:210:119-132. PMID: 37494784
Biomed Res Int

TAK-242 Ameliorates Hepatic Fibrosis by Regulating the Liver-Gut Axis. [Abstract]

2022 Aug 16:2022:4949148. PMID: 36017390
PeerJ

The immunostimulatory activity of polysaccharides from Glycyrrhiza uralensis. [Abstract]

2020 Jan 29;8:e8294. PMID: 32030319
Toxicol Res (Camb)

Inhibitions of HMGB1 and TLR4 alleviate DINP-induced asthma in mice. [Abstract]

2019 Jun 18;8(5):621-629. PMID: 31588340
Vet Microbiol

FAdV-4-induced secondary Pasteurella multocida infection potentiates bacterial adherence and aggravates pathological damage in SPF chickens. [Abstract]

2026 Apr:315:110959. PMID: 41764915
Hum Cell

SerpinB1 reduces neutrophil airway inflammation, airway remodeling, and pyroptosis in asthmatic mice by interacting with Elane. [Abstract]

2025 Oct 31;38(6):183. PMID: 41171365
Mol Cell Biol

miR-365-3p Regulates Gastrointestinal Dysfunction in Diabetes Mellitus Rats via the TLR4/MyD88/NF-κB Pathway. [Abstract]

2025 Jul 22:1-17. PMID: 40693422
Physiol Res

Baicalin alleviates silica-induced lung inflammation and fibrosis by inhibiting TLR4/NF-?B pathway in rats. [Abstract]

2023 Apr 30;72(2):221-233. PMID: 37159856
Brain Behav

Effect of Toll-like receptor 4 on depressive-like behaviors induced by chronic social defeat stress. [Abstract]

2020 Mar;10(3):e01525. PMID: 31945269
Vet Microbiol

Mycoplasma hyopneumoniae Mhp597 is a cytotoxicity, inflammation and immunosuppression associated nuclease. [Abstract]

2019 Aug:235:53-62. PMID: 31282379
Vet Microbiol

Dendritic cell-targeted recombinantLactobacilli induce DC activation and elicit specific immune responses against G57 genotype of avian H9N2 influenza virus infection. [Abstract]

2018 Sep:223:9-20. PMID: 30173758
PLoS One

Immunostimulatory activity of water-extractable polysaccharides from Cistanche deserticola as a plant adjuvant in vitro and in vivo. [Abstract]

2018 Jan 23;13(1):e0191356. PMID: 29360858
Graefes Arch Clin Exp Ophthalmol

Inhibition of TLR4 alleviates the inflammation and apoptosis of retinal ganglion cells in high glucose. [Abstract]

2017 Nov;255(11):2199-2210. PMID: 28808786

Resatorvid purchased from MedChemExpress. Usage Cited in: Graefes Arch Clin Exp Ophthalmol. 2017 Nov;255(11):2199-2210. [Abstract]

The effect of TAK-242 on the expression levels of NF-κB and MyD88 in retinal ganglion cells (RGCs) under high glucose are detected by Western blotting.

Resatorvid purchased from MedChemExpress. Usage Cited in: Graefes Arch Clin Exp Ophthalmol. 2017 Nov;255(11):2199-2210. [Abstract]

The effect of TAK-242 on the expression levels of TRAF6 and NLRP3 in retinal ganglion cells (RGCs) under high glucose are detected by Western blotting.
PLoS One

The N-terminal region of serum amyloid A3 protein activates NF-κB and up-regulates MUC2 mucin mRNA expression in mouse colonic epithelial cells. [Abstract]

2017 Jul 24;12(7):e0181796. PMID: 28738073
PLoS One

Upregulation of TLR4 via PKC activation contributes to impaired wound healing in high-glucose-treated kidney proximal tubular cells. [Abstract]

2017 May 24;12(5):e0178147. PMID: 28542370

Resatorvid purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 May 24;12(5):e0178147. [Abstract]

(A) Titration of TAK-242 concentration. RPTC cells are cultured for 12 h in low glucose or high glucose medium with or without TAK-242. (B) MyD88 upregulation is also inhibited by TAK-242 under high glucose conditions by Western blotting.
Vet Microbiol

Newcastle disease virus-like particles induce DC maturation through TLR4/NF-κB pathway and facilitate DC migration by CCR7-CCL19/CCL21 axis. [Abstract]

2017 May:203:158-166. PMID: 28619138
PLoS One

TAK-242, a Toll-Like Receptor 4 Antagonist, Protects against Aldosterone-Induced Cardiac and Renal Injury. [Abstract]

2015 Nov 10;10(11):e0142456. PMID: 26556241

Resatorvid purchased from MedChemExpress. Usage Cited in: PLoS One. 2015 Nov 10;10(11):e0142456. [Abstract]

Renal protein expression of E-cadherin (an epithelial marker), and Fibronectin and a-SMA (mesenchymal markers) are assayed in rats treated with Aldo-salt or with Aldo-salt plus TAK-242. TAK-242 reverses the Aldo-salt-induced renal epithelial-mesenchymal transition.
BMC Musculoskelet Disord

Immune response associated with Toll-like receptor 4 signaling pathway leads to steroid-induced femoral head osteonecrosis. [Abstract]

2014 Jan 15;15(1):18. PMID: 24428851
Int J Med Microbiol

Cronobacter sakazakii induces necrotizing enterocolitis by regulating NLRP3 inflammasome expression via TLR4. [Abstract]

2020 May;69(5):748-758. PMID: 32209170
J Mol Histol

HMGB1 promotes intracranial aneurysm progression by regulating vascular smooth muscle cell phenotypic switching and ferroptosis. [Abstract]

2026 Jun 8;57(3):190. PMID: 42257786
Am J Physiol Regul Integr Comp Physiol

Liraglutide ameliorates inflammation and fibrosis by downregulating the TLR4/MyD88/NF-kappaB pathway in diabetic kidney disease. [Abstract]

2024 Oct 1;327(4):R410-R422. PMID: 39133777
Burns

Heme oxygenase-1 induction mitigates burn-associated early acute kidney injury via the TLR4 signaling pathway. [Abstract]

2022 Feb;48(1):156-167. PMID: 33962830
J Pept Sci

Identification of a targeting-delivery peptide based on rhCNB. [Abstract]

2019 Jun;25(6):e3159. PMID: 30843319
Photochem Photobiol

Resatorvid-based Pharmacological Antagonism of Cutaneous TLR4 Blocks UV-induced NF-κB and AP-1 Signaling in Keratinocytes and Mouse Skin. [Abstract]

2016 Nov;92(6):816-825. PMID: 27859308

Resatorvid purchased from MedChemExpress. Usage Cited in: Photochem Photobiol. 2016 Nov;92(6):816-825. [Abstract]

Western blot analysis reveals that Resatorvid-based inhibition of TLR4 is able to block UV-induced phosphorylation of MAP kinases (p38 and JNK) and Akt.
Clin Exp Pharmacol Physiol

Targeting S100A8/A9 Ameliorates Heart Failure with Preserved Ejection Fraction by Modulating TLR4/NF-κB-Mediated Inflammation. [Abstract]

2026 Jun;53(6):e70140. PMID: 42264451
Eur J Neurosci

Systematic analysis of critical genes and pathways identified a signature of neuropathic pain after spinal cord injury. [Abstract]

2022 Jul;56(2):3991-4008. PMID: 35560852
Biochem Biophys Res Commun

Uric acid inhibits HMGB1-TLR4-NF-κB signaling to alleviate oxygen-glucose deprivation/reoxygenation injury of microglia. [Abstract]

2021 Feb 12:540:22-28. PMID: 33429196
Med Sci Monit

Ability of Post-treatment Glycyrrhizic Acid to Mitigate Cerebral Ischemia/Reperfusion Injury in Diabetic Mice. [Abstract]

2020 Sep 28:26:e926551. PMID: 32981927
Biotechnol Lett

Recombinant ferritin nanoparticles can induce dendritic cell maturation through TLR4/NF-κB pathway. [Abstract]

2020 Dec;42(12):2489-2500. PMID: 32567013
Cell Physiol Biochem

Effects of the TLR4/Myd88/NF-κB Signaling Pathway on NLRP3 Inflammasome in Coronary Microembolization-Induced Myocardial Injury. [Abstract]

2018;47(4):1497-1508. PMID: 29940584

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;47(4):1497-1508. [Abstract]

TAK-242 inhibits coronary microembolization (CME)-induced TLR4 upregulation and NLRP3 inflammasome activation.
Cell Physiol Biochem

TAK-242 Protects Against Apoptosis in Coronary Microembolization-Induced Myocardial Injury in Rats by Suppressing TLR4/NF-κB Signaling Pathway. [Abstract]

2017;41(4):1675-1683. PMID: 28359050

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1675-1683. [Abstract]

TLR4 protein expression detected by western blot.

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1675-1683. [Abstract]

MyD88 protein expression detected by western blot.

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1675-1683. [Abstract]

NF-κB p65 (nuclei) protein expression detected by western blot.

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1675-1683. [Abstract]

p-IκBα protein expression detected by western blot.

Resatorvid purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1675-1683. [Abstract]

Cleaved caspase-3 protein expression detected by western blot.
FASEB Bioadv

Endoplasmic Reticulum Stress and Unfolded Protein Response Sensor ERN1 Regulates Organic Dust Induction of Lung Inflammation. [Abstract]

2025 Jul 9;7(7):e70031. PMID: 40641847
J Mol Neurosci

MiR-124 Prevents the Microglial Proinflammatory Response by Inhibiting the Activities of TLR4 and Downstream NLRP3 in Palmitic Acid-Treated BV2 Cells. [Abstract]

2022 Mar;72(3):496-506. PMID: 34652636
Microcirculation

Post-treatment with yiqifumai injection and its main ingredients attenuates lipopolysaccharide-induced microvascular disturbance in mesentery and ileum. [Abstract]

2021 May;28(4):e12680. PMID: 33486837
Scand J Immunol

Saturated fatty acids activate the inflammatory signalling pathway in Schwann cells: Implication in sciatic nerve injury. [Abstract]

2020 Aug;92(2):e12896. PMID: 32557749
J Mol Neurosci

Translocation Associated Membrane Protein 1 Contributes to Chronic Constriction Injury-Induced Neuropathic Pain in the Dorsal Root Ganglion and Spinal Cord in Rats. [Abstract]

2018 Dec;66(4):535-546. PMID: 30338452

Resatorvid purchased from MedChemExpress. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546. [Abstract]

The increasing of TRAM1 is reversed by TAK242.

Resatorvid purchased from MedChemExpress. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546. [Abstract]

In SC, p-NF-κB production is inhibited by TRAM1 siRNA or TAK242.

Resatorvid purchased from MedChemExpress. Usage Cited in: J Mol Neurosci. 2018 Dec;66(4):535-546. [Abstract]

In DRG, p-NF-κB production is inhibited by TRAM1 siRNA or TAK242.
J Biochem

Adiponectin suppression of late inflammatory mediator, HMGB1-induced cytokine expression in RAW264 macrophage cells. [Abstract]

2018 Feb 1;163(2):143-153. PMID: 29048484
J Thorac Dis

Yanghepingchuan granule improves airway inflammation by inhibiting autophagy via miRNA328-3p/high mobility group box 1/Toll-like receptor 4 targeting of the pathway of signaling in rat models of asthma. [Abstract]

2023 Nov 30;15(11):6251-6264. PMID: 38090296
J Food Biochem

Walnut oil alleviates LPS-induced intestinal epithelial cells injury by inhibiting TLR4/MyD88/NF-κB pathway activation. [Abstract]

2021 Nov;45(11):e13955. PMID: 34580887
Acta Otorhinolaryngol Ital

Dose-dependent IL-29 activation of TLR4 signalling drives eosinophil infiltration in chronic rhinosinusitis with nasal polyps. [Abstract]

2026 Apr;46(2):128-138. PMID: 42041069
J Oral Biosci

Neisseria perflava isolated from a clinical sample reduces influenza virus replication in respiratory cells. [Abstract]

2025 Apr 23:100665. PMID: 40280275
Exp Ther Med

Bilobalide attenuates lipopolysaccharide‑induced HepG2 cell injury by inhibiting TLR4‑NF‑κB signaling via the PI3K/Akt pathway. [Abstract]

2023 Nov 22;27(1):24. PMID: 38125341
Exp Ther Med

Dexmedetomidine-mediated regulation of miR-17-3p in H9C2 cells after hypoxia/reoxygenation injury. [Abstract]

2020 Aug;20(2):917-925. PMID: 32742334
Exp Ther Med

miR-34a alleviates spinal cord injury via TLR4 signaling by inhibiting HMGB-1. [Abstract]

2019 Mar;17(3):1912-1918. PMID: 30783468
Neurosci Lett

TLR4 signaling pathway mediates the LPS/ischemia-induced expression of monocytechemotactic protein-induced protein 1 in microglia. [Abstract]

2018 Nov 1:686:33-40. PMID: 30179651

Resatorvid purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2018 Nov 1:686:33-40. [Abstract]

Western Blot analyses show the protein expression of MCPIP1 after the treatment of PBS and LPS (with TAK-242, C29, FPS-ZM1).

Resatorvid purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2018 Nov 1:686:33-40. [Abstract]

Images show the expression of MCPIP1 after the treatment of of PBS and LPS (with TAK-242, C29, FPS-ZM1).
Cytotechnology

Immunostimulatory effect of dried bonito extract on mouse macrophage cell lines and mouse primary peritoneal macrophages. [Abstract]

2017 Apr;69(2):229-244. PMID: 28084562
Oncol Lett

Hypoxia-inducible factor-1α mediates the toll-like receptor 4 signaling pathway leading to anti-tumor effects in human hepatocellular carcinoma cells under hypoxic conditions. [Abstract]

2016 Aug;12(2):1034-1040. PMID: 27446390

Resatorvid purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2016 Aug;12(2):1034-1040. [Abstract]

Involvement of TLR4 signaling pathway in HIF-1α silencing affects inflammatory and apoptosis under hypoxic conditions. In total, 30 mg total lysate is harvested with radioimmunoprecipitation assay buffer to detect TLR4, HIF-1α, caspase-3, MyD88, p-ASK1 and p-p38 protein expression by western blot analysis in human hepatocellular carcinoma HepG2 cells. The expression of TLR4, HIF-1α, MyD88, p-ASK1 NS and p-p38 in shHIF-1α transfected cells is significantly higher compared with the parental cells.
Growth Factors

Effects of penehyclidine hydrochloride on myocardial ischaemia-reperfusion injury in rats by inhibiting TLR4/MyD88/NF-κB pathway via miR-199a-3p. [Abstract]

2022 Nov;40(5-6):186-199. PMID: 35984706
J Interferon Cytokine Res

Induction of Chemokines by Hepatitis C Virus Proteins: Synergy of the Core Protein with Interleukin-1β and Interferon-γ in Liver Bystander Cells. [Abstract]

2020 Apr;40(4):195-206. PMID: 32031878
J Vet Sci

Subcutaneous Streptococcus dysgalactiae GAPDH vaccine in mice induces a proficient innate immune response. [Abstract]

2023 Sep;24(5):e72. PMID: 38031651
Am J Transl Res

Rehabilitation training inhibits neuronal apoptosis by down-regulation of TLR4/MyD88 signaling pathway in mice with cerebral ischemic stroke. [Abstract]

2021 Apr 15;13(4):2213-2223. PMID: 34017384
Stem Cells Cloning

Novel, Reproducible, Consortia Factors Derived from Adipose Stem Cells for Burn Wound Treatment. [Abstract]

2025 Jun 6:18:63-72. PMID: 40495998
Curr Eye Res

TLR4/TRIF/Caspase-8/Caspase-1 Pathway in Choroidal Endothelial Cells Promotes Choroidal Neovascularization. [Abstract]

2025 Feb;50(2):203-212. PMID: 39392113
J Asian Nat Prod Res

The mechanism of Yizhi Qingxin formula to improve neuroinflammation in Alzheimer's disease by regulating the TLR4/NF‑κB/NLRP3 pathway. [Abstract]

2025 Aug 4:1-19. PMID: 40757693
Toxicol Ind Health

Ambient fine particulate matter induces inflammatory responses of vascular endothelial cells through activating TLR-mediated pathway. [Abstract]

2019 Oct;35(10):670-678. PMID: 31601156
Chem Pharm Bull

MiR-135a Protects against Myocardial Injury by Targeting TLR4. [Abstract]

2021;69(6):529-536. PMID: 34078799
Biosci Biotechnol Biochem

Immunostimulatory effect of spinach aqueous extract on mouse macrophage-like J774.1 cells and mouse primary peritoneal macrophages. [Abstract]

2016 Jul;80(7):1393-402. PMID: 27095137
Transfus Clin Biol

TLR4/MD-2 complex promotes transfusion-related acute lung injury pathogenesis through the activation of the AP-1 and NF-κB signaling pathways. [Abstract]

2026 Jun 24:S1246-7820(26)00097-2. PMID: 42341909
Drug Discov Ther

A single dose of ketamine relieves fentanyl-induced-hyperalgesia by reducing inflammation initiated by the TLR4/NF-κB pathway in rat spinal cord neurons. [Abstract]

2023 Sep 15;17(4):279-288. PMID: 37558466
Ann Transplant

Toll-Like Receptor 3 Activator Preconditioning Enhances Modulatory Function of Adipose‑Derived Mesenchymal Stem Cells in a Fully MHC-Mismatched Murine Model of Heterotopic Heart Transplantation. [Abstract]

2020 May 5;25:e921287. PMID: 32366814
Transfus Apher Sci

Haemin-induced cell death in human monocytic cells is consistent with ferroptosis. [Abstract]

2018 Aug;57(4):524-531. PMID: 29859670
Eur J Inflamm

2021 May 17.
J Carbohydr Chem

15 Sep 2021.
SSRN

2026 May 12.
SSRN

2026 Apr 28.
SSRN

2026 Apr 7.
Patent

US20260034087A1.
medRxiv

2025 Dec 19.
University of Sao Paulo

2025.
SSRN

2025 Nov 11.
Biomed Pharmacother

Baicalin attenuates acetaminophen-induced acute liver injury through inhibiting TLR2-dependent neutrophil extracellular trap formation. [Abstract]

2025 Sep 17:192:118569. PMID: 40967078
Stanford University

2025.
SSRN

2025 Jun 2.
bioRxiv

2025 April 16.
SSRN

2025 Apr 13.
bioRxiv

2025 March 13.
bioRxiv

2025 March 10.
SSRN

2025 Feb 26.
SSRN

2025 Mar 17.
Brain Behav Immun Integr

2025 Jan.
Drexel University

2025.
Res Sq

2024 Aug 20.
Res Sq

2024 Oct 10.
University of Oregon

2024.
SSRN

2024 Apr 4.
bioRxiv

2024 July 03.
Research Square Preprint

2023 Dec 29.
Research Square Preprint

2024 Jan 24.
Preprints

2023 Dec 12.
Preprints

2023 Dec 26.
SSRN

2023 Nov 3.
Sci Tradit Chin Med

2023 Sep 20.
SSRN

2023 Sep 6.
Biomed Pharmacother

The antimicrobial peptide chensinin-1b alleviates the inflammatory response by targeting the TLR4/NF-κB signaling pathway and inhibits Pseudomonas aeruginosa infection and LPS-mediated sepsis. [Abstract]

2023 Sep:165:115227. PMID: 37536032
University of Bonn

2023 May 31.
bioRxiv

Vascular Endothelial-derived SPARCL1 Exacerbates Viral Pneumonia Through Pro-Inflammatory Macrophage Activation. [Abstract]

2023 May 25:2023.05.25.541966. PMID: 37292817
Research Square Preprint

2023 Apr 3.
Heliyon

An active fraction from Spatholobus suberectus dunn inhibits the inflammatory response by regulating microglia activation, switching microglia polarization from M1 to M2 and suppressing the TLR4/MyD88/NF-κB pathway in LPS-stimulated BV2 cells. [Abstract]

2023 Mar 30;9(4):e14979. PMID: 37064439
Biomed Pharmacother

Immunoregulatory effects of Tetrastigma hemsleyanum polysaccharide via TLR4-mediated NF-κB and MAPK signaling pathways in Raw264.7 macrophages. [Abstract]

2023 May:161:114471. PMID: 36889110
Environ Toxicol

Triphenyl phosphate-induced macrophages dysfunction by activation TLR4-mediated ERK/NF-κB pathway. [Abstract]

2023 Jul;38(7):1484-1493. PMID: 36929861
Patent

US20230058557A1.
Biomed Pharmacother

Polysaccharides from Tetrastigma Hemsleyanum Diels et Gilg attenuate LPS-induced acute lung injury by modulating TLR4/COX-2/NF-κB signaling pathway. [Abstract]

2022 Nov:155:113755. PMID: 36182735
Evid Based Complement Alternat Med

Synergistic Effect of Polydatin and Polygonatum sibiricum Polysaccharides in Combating Atherosclerosis via Suppressing TLR4-Mediated NF- κ B Activation in ApoE-Deficient Mice. [Abstract]

2022 Jul 7:2022:3885153. PMID: 35845572
Contrast Media Mol Imaging

Toll-Like Receptor 4 Exacerbates Mycoplasma pneumoniae via Promoting Transcription Factor EB-Mediated Autophagy. [Abstract]

2022 Jul 31:2022:3357694. PMID: 35965629
Oxid Med Cell Longev

TLR4-SIRT3 Mechanism Modulates Mitochondrial and Redox Homeostasis and Promotes EPCs Recruitment and Survival. [Abstract]

2022 Jul 4:2022:1282362. PMID: 35832490
Research Square Print

2022 Jun.
Oxid Med Cell Longev

Tumor Necrosis Factor- α-Induced Protein 8-Like 2 Ameliorates Cardiac Hypertrophy by Targeting TLR4 in Macrophages. [Abstract]

2022 Apr 26;2022:9469143. PMID: 35528518
Research Square Preprint

2022 May.
Oxid Med Cell Longev

Isoflurane Attenuates Cerebral Ischaemia-Reperfusion Injury via the TLR4-NLRP3 Signalling Pathway in Diabetic Mice. [Abstract]

2022 Apr 4;2022:2650693. PMID: 35419168
Oxid Med Cell Longev

Advanced Glycation End Products Induce Atherosclerosis via RAGE/TLR4 Signaling Mediated-M1 Macrophage Polarization-Dependent Vascular Smooth Muscle Cell Phenotypic Conversion. [Abstract]

2022 Jan 13:2022:9763377. PMID: 35069982
Research Square Preprint

2021 Dec.
Research Square Preprint

2021 Dec.
Research Square Preprint

2021 Oct.
SSRN

20 Oct 2021.
Oxid Med Cell Longev

Recombinant High-Mobility Group Box 1 (rHMGB1) Promotes NRF2-Independent Mitochondrial Fusion through CXCR4/PSMB5-Mediated Drp1 Degradation in Endothelial Cells. [Abstract]

2021 Aug 2;2021:9993240. PMID: 34394840
Université catholique de Louvain

2021 Aug.
Research Square Preprint

2021 Jul.
Research Square Preprint

2021 May.
Research Square Preprint

2021 Mar.
Oxid Med Cell Longev

Resveratrol Confers Vascular Protection by Suppressing TLR4/Syk/NLRP3 Signaling in Oxidized Low-Density Lipoprotein-Activated Platelets. [Abstract]

2021 Feb 25:2021:8819231. PMID: 33728029
Research Square Preprint

2021 Jan.
Research Square Preprint

2021 Jan.
Research Square Preprint

2020 Dec.
Research Square Preprint

2020 Dec.
Research Square Preprint

2020 Jul.
Biomed Pharmacother

Xijiao Dihuang decoction improves prognosis of sepsis via inhibition of aerobic glycolysis. [Abstract]

2020 Sep;129:110501. PMID: 32768976
Research Square Preprint

2020 May.
Oxid Med Cell Longev

High-Fat Diet Aggravates Acute Pancreatitis via TLR4-Mediated Necroptosis and Inflammation in Rats. [Abstract]

2020 Jan 8;2020:8172714. PMID: 31998444
Biomed Pharmacother

Immunomodulatory effects exerted by Poria Cocos polysaccharides via TLR4/TRAF6/NF-κB signaling in vitro and in vivo. [Abstract]

2019 Apr:112:108709. PMID: 30970514
Oxid Med Cell Longev

Triptolide Inhibits Preformed Fibril-Induced Microglial Activation by Targeting the MicroRNA155-5p/SHIP1 Pathway. [Abstract]

2019 Apr 28:2019:6527638. PMID: 31182996
University of Eastern Finland

2019 Apr.
J Biomed Nanotechnol

Fine Particulate Matter (PM2.5) Promoted the Invasion of Lung Cancer Cells via an ARNT2/PP2A/STAT3/MMP2 Pathway. [Abstract]

2018 Dec 1;14(12):2172-2184. PMID: 30305224
mustansiriya medical journal

2018, 17(2):85.
Patent

US20180177918A1.
Oxid Med Cell Longev

The Role of TLR4 on PGC-1 α-Mediated Oxidative Stress in Tubular Cell in Diabetic Kidney Disease. [Abstract]

2018 May 16:2018:6296802. PMID: 29861832

Resatorvid purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2018 May 16:2018:6296802. [Abstract]

HK-2 cells are treated with TLR4 inhibitor (TAK242, 5 μM) for 2 h prior to HG (30 mM) treatment for 2 h and with NF-κB blocker (Parthenolide, 10 μM) and HG (30 mM) for 2 h, and the samples are collected for Western blot analysis.
China Journal of Modern Medicine

Feb 2018.
University of Arizona

2017 Nov.
Hainan Med J, Aug

2017, Vol. 28, No. 15.
Oncotarget

λ-Carrageenan improves the antitumor effect of dendritic cellbased vaccine. [Abstract]

2017 May 2;8(18):29996-30007. PMID: 28404904
Universität Würzburg

2017 May 9.
Oncotarget

Invasive Fusobacterium nucleatum activates beta-catenin signaling in colorectal cancer via a TLR4/P-PAK1 cascade. [Abstract]

2017 May 9;8(19):31802-31814. PMID: 28423670

Resatorvid purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 9;8(19):31802-31814. [Abstract]

Activation of the β-catenin signaling pathway by Fn (F01) can be inhibited by both the TLR4 inhibitor (TAK-242) and PAK1 inhibitor (IPA-3).
Oncotarget

Relaxin abrogates renal interstitial fibrosis by regulating macrophage polarization via inhibition of Toll-like receptor 4 signaling. [Abstract]

2017 Mar 28;8(13):21044-21053. PMID: 28416741
Chinese Journal of Public Health

2016,32(11):1480-1484.
Seitoku University

2014.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (276.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 20 mg/mL (55.28 mM; Need ultrasonic and warming)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7638 mL

13.8190 mL

27.6381 mL

5 mM

0.5528 mL

2.7638 mL

5.5276 mL

10 mM

0.2764 mL

1.3819 mL

2.7638 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 5.5 mg/mL (15.20 mM); Suspended solution; Need ultrasonic

Protocol 3

Add each solvent one by one: 10% DMSO 90% Saline

Solubility: 5 mg/mL (13.82 mM); Suspended solution; Need ultrasonic

Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.75 mg/mL (7.60 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (7.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 7

Add each solvent one by one: 5% DMSO 95% Saline

Solubility: 2.5 mg/mL (6.91 mM); Suspended solution; Need ultrasonic

Protocol 8

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: 0.5 mg/mL (1.38 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ii M, et al. A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling. [Content Brief]

[2]. Yamada M, et al. Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J Med Chem. 2005 Nov 17;48(23):7457-67. [Content Brief]

[3]. Yuko Ono, et al. TAK-242, a Specific Inhibitor of Toll-like Receptor 4 Signalling, Prevents Endotoxemia-Induced Skeletal Muscle Wasting in Mice. Sci Rep. 2020 Jan 20;10(1):694. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.7638 mL	13.8190 mL	27.6381 mL	69.0951 mL
	5 mM	0.5528 mL	2.7638 mL	5.5276 mL	13.8190 mL
	10 mM	0.2764 mL	1.3819 mL	2.7638 mL	6.9095 mL
	15 mM	0.1843 mL	0.9213 mL	1.8425 mL	4.6063 mL
	20 mM	0.1382 mL	0.6910 mL	1.3819 mL	3.4548 mL
	25 mM	0.1106 mL	0.5528 mL	1.1055 mL	2.7638 mL
	30 mM	0.0921 mL	0.4606 mL	0.9213 mL	2.3032 mL
	40 mM	0.0691 mL	0.3455 mL	0.6910 mL	1.7274 mL
	50 mM	0.0553 mL	0.2764 mL	0.5528 mL	1.3819 mL
DMSO	60 mM	0.0461 mL	0.2303 mL	0.4606 mL	1.1516 mL
	80 mM	0.0345 mL	0.1727 mL	0.3455 mL	0.8637 mL
	100 mM	0.0276 mL	0.1382 mL	0.2764 mL	0.6910 mL

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Product Name:
CAS No.:
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Resatorvid

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Membrane Protein-targeted Compound Library

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Highly Selective Inhibitors Library

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Bioactive Compound Library

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Anti-Brain Cancer Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) Resatorvid

All Toll-like Receptor (TLR) Isoforms

All TNF Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Publications (524)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Resatorvid Related Classifications

HY-11109 Related Classifications