TLR4-IN-C34
Based on 14 publication(s) in Google Scholar
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 40592-88-9
- Formula: C17H27NO9
- Molecular Weight:389.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) TLR4-IN-C34
More- Gut Microbes. 2025 Dec;17(1):2471015. [Abstract]
- Cell Commun Signal. 2025 Aug 26;23(1):381. [Abstract]
- Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
- EMBO J. 2021 May 17;40(10):e106188. [Abstract]
- Sci Total Environ. 2024 Dec 10:955:177132. [Abstract]
- Environ Pollut. 2025 Oct 1:382:126762. [Abstract]
- Int J Mol Sci. 2024 Mar 27;25(7):3735. [Abstract]
- Front Pharmacol. 2022 Jul 22;13:920928. [Abstract]
- Int Immunopharmacol. 2024 Dec 25:146:113938. [Abstract]
- Eur J Pharmacol. 2022 Nov 5:934:175294. [Abstract]
- Sci Rep. 2023 Nov 9;13(1):19440. [Abstract]
- Cell Signal. 2025 Aug 23:136:112084. [Abstract]
- Toxicol Appl Pharmacol. 2025 Jan 18:117232. [Abstract]
- bioRxiv. 2026 Mar 20.
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In Vivo Efficacy Study
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Cell Migration/Invasion Assay
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Cell Migration/Invasion Assay
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WB
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WB
Biological Activity
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TLR4 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Experimental NEC induced in 7-8 day old mice[1].
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Dosage:1 mg/kg.
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Administration:Orally every morning.
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Result:Attenuated intestinal inflammation.
Chemical Information
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CAS No. 40592-88-9
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Appearance Solid
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Molecular Weight 389.40
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Formula C17H27NO9
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Color White to off-white
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SMILES
O=C(N[C@H]([C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O1)[C@H]1OC(C)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Gut Microbes
Gut microbial dysbiosis exacerbates long-term cognitive impairments by promoting intestinal dysfunction and neuroinflammation following neonatal hypoxia-ischemia. [Abstract]2025 Dec;17(1):2471015. PMID: 40008452
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2471015. [Abstract]
TLR4-IN-C34 ( orally; 1 mg/kg daily from the 7th postnatal day to the 3rd day after HI insult) treatment improved intestinal dysfunction and alleviated synaptic and cognitive impairments in the neonatal HIBD rats. The expression levels of TLR4 of colon by WB and IF analyses.
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Cell Commun Signal
2025 Aug 26;23(1):381. PMID: 40859363
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381. [Abstract]
Neutrophils were pretreated with the TLR2 and TLR4 inhibitor Sparstolonin B (SsnB) (HY-116213; 10 µM), the TLR2 inhibitor C29 (HY-100461; 100 µM), or the TLR4 inhibitor C34 (TLR4-IN-C34; HY-107575; 10 µM) for 30 min before stimulation with calreticulin. Transwell migration assay. The lower chambers were loaded with blank culture medium (a), calreticulin (b), calreticulin with SsnB (c), calreticulin with C29 (d), or calreticulin with C34 (e). CFSE-labeled neutrophils were loaded into the upper chamber and allowed to migrate for 3 h.
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381. [Abstract]
Neutrophils were pretreated with the TLR2 and TLR4 inhibitor Sparstolonin B (SsnB) (HY-116213; 10 µM), the TLR2 inhibitor C29 (HY-100461; 100 µM), or the TLR4 inhibitor C34 (TLR4-IN-C34; HY-107575; 10 µM) for 30 min before stimulation with calreticulin. F-actin was detected for 30 min the incubation of neutrophils with calreticulin in the presence of the respective inhibitors (scale bars = 10 μm).
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Aug 26;23(1):381. [Abstract]
Neutrophils were incubated in calreticulin with or without inhibitors of TLR2/TLR4 (SsnB; HY-116213; 10 µM), TLR2 (C29; HY-100461; 100 µM), or TLR4 (C34; TLR4-IN-C34; HY-107575; 10 µM) for 0 min, 1 min, 3 min, or 5 min. The cell lysate was prepared and subjected to western blotting for analysis of the expression of Cdc42, Rac1, and RhoA. Densitometric analysis of each protein band is shown below the blots, representing grayscale quantification relative to internal controls
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Cell Commun Signal
Neutrophil extracellular traps induced by the hypoxic microenvironment in gastric cancer augment tumour growth. [Abstract]2023 May 1;21(1):86. PMID: 37127629
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the p-p38 level in neutrophils was measured by western blotting.
TLR4-IN-C34 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the NET formation was detected with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm. All values are the means ± SDs. ns = not significant, **P < 0.01
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EMBO J
2021 May 17;40(10):e106188. PMID: 33881780 -
Sci Total Environ
Water pollutant cadmium-induced intestinal inflammation in Eriocheir sinensis and potential therapeutic drugs. [Abstract]2024 Dec 10:955:177132. PMID: 39442721 -
Environ Pollut
Silica-induced innate immune activation drives macrophage pyroptosis and lung inflammation through glycolytic reprogramming. [Abstract]2025 Oct 1:382:126762. PMID: 40614958 -
Int J Mol Sci
The Tumor Microenvironment Mediates the HIF-1α/PD-L1 Pathway to Promote Immune Escape in Colorectal Cancer. [Abstract]2024 Mar 27;25(7):3735. PMID: 38612546 -
Front Pharmacol
Nucleotide-Binding Oligomerization Domain 1/Toll-Like Receptor 4 Co-Engagement Promotes Non-Specific Immune Response Against K562 Cancer Cells. [Abstract]2022 Jul 22;13:920928. PMID: 35935855 -
Int Immunopharmacol
2024 Dec 25:146:113938. PMID: 39724736 -
Eur J Pharmacol
Pharmacological inhibition of toll-like receptor 4 with TLR4-IN-C34 modulates the intestinal flora homeostasis and the MyD88/NF-κB axis in ulcerative colitis. [Abstract]2022 Nov 5:934:175294. PMID: 36152840 -
Sci Rep
Dysfunctional TLR1 reduces the therapeutic efficacy of chemotherapy by attenuating HMGB1-mediated antitumor immunity in locally advanced colorectal cancer. [Abstract]2023 Nov 9;13(1):19440. PMID: 37945630 -
Cell Signal
TLR4-IN-C34 attenuates the progression of osteoarthritis through inhibiting inflammation, angiogenesis and pain. [Abstract]2025 Aug 23:136:112084. PMID: 40854507 -
Toxicol Appl Pharmacol
T-2 toxin triggers immunotoxic effects in goats by inducing ferroptosis and neutrophil extracellular traps. [Abstract]2025 Jan 18:117232. PMID: 39832565 -
Solvent & Solubility
DMSO : 200 mg/mL (513.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 33.33 mg/mL (85.59 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.84 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (12.84 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 7.69 mg/mL (19.75 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Neal MD, et al. Discovery and validation of a new class of small molecule Toll-like receptor 4 (TLR4) inhibitors. PLoS One. 2013 Jun 12;8(6):e65779. [Content Brief]
[2]. Wipf P, et al. Synthesis of anti-inflammatory α-and β-linked acetamidopyranosides as inhibitors of toll-like receptor 4 (TLR4). Tetrahedron Lett. 2015 Jun 3;56(23):3097-3100. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL | 64.2013 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL | 12.8403 mL | |
| 10 mM | 0.2568 mL | 1.2840 mL | 2.5681 mL | 6.4201 mL | |
| 15 mM | 0.1712 mL | 0.8560 mL | 1.7120 mL | 4.2801 mL | |
| 20 mM | 0.1284 mL | 0.6420 mL | 1.2840 mL | 3.2101 mL | |
| 25 mM | 0.1027 mL | 0.5136 mL | 1.0272 mL | 2.5681 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8560 mL | 2.1400 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6420 mL | 1.6050 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5136 mL | 1.2840 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0700 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8025 mL | |
| DMSO | 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6420 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.