C34 (Synonyms: Toll-Like Receptor 4-C34) |
Catalog No.GC11275
One-Click Copy Product Info
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C34 is an orally active, selective Toll-like receptor 4 (TLR4) antagonist. C34 exerts anti-inflammatory effects by inhibiting the TLR4/MyD88/NF-κB signaling pathway, thereby reducing the production of pro-inflammatory cytokines.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 40592-88-9
Sample solution is provided at 25 µL, 10mM.
C34 is an orally active, selective Toll-like receptor 4 (TLR4) antagonist. C34 exerts anti-inflammatory effects by inhibiting the TLR4/MyD88/NF-κB signaling pathway, thereby reducing the production of pro-inflammatory cytokines[1-2]. C34 alleviates systemic inflammation in various disease models, including endotoxemia, necrotizing enterocolitis, ulcerative colitis, and acute kidney injury. TLR4-IN-C34 is applicable for research in immunology, inflammation, and related disorders[3-4].
In vitro, BV2 microglial cells were pretreated with C34 (10-100μM) for 2 hours, followed by LPS (200ng/mL) stimulation for 24 hours. C34 significantly inhibited LPS-induced activation of the TLR4/MyD88/NF-κB signaling pathway, downregulated the release of pro-inflammatory factors (TNF-α, IL-1β, IL-6, MCP-1, and NO), and reduced ROS generation and NLRP3 inflammasome activation[5]. Rat enteric glial cells were pretreated with C34 (50μM) for 1 hour, then exposed to Clostridioides difficile toxins TcdA (50ng/mL) or TcdB (1ng/mL) for 18 hours. C34 significantly suppressed toxin-induced TLR4/NF-κB p65 nuclear translocation and TNF-α protein expression, and decreased apoptosis[6].
In vivo, in an isoprenaline (ISO; 100mg/kg)-induced Wistar rat model, C34 (1mg/kg or 3mg/kg; administered intraperitoneally 1 hour before each of two ISO injections), C34 significantly reduced serum creatinine levels and ameliorated renal tissue inflammation, fibrosis, and apoptosis[7]. In a Pilocarpine (40mg/kg; i.p.)-induced status epilepticus Wistar rat model, C34 (1μg/rat; single intracerebroventricular injection) was administered 1 hour or 24 hours after pilocarpine injection. Administration at 1 hour post-induction, C34 significantly reduced hippocampal neuronal death, decreased levels of the apoptotic factor caspase-3 and inflammatory mediators TNF-α and NF-κB, whereas treatment at 24 hours, C34 showed a markedly diminished therapeutic effect[8].
References:
[1] Wipf P, Eyer BR, Yamaguchi Y, 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.
[2] Neal MD, Jia H, Eyer B, 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.
[3] Wei K, Zou Y, Xu H, et al. TLR4-IN-C34 attenuates the progression of osteoarthritis through inhibiting inflammation, angiogenesis and pain. Cell Signal. 2025 Dec;136:112084.
[4] Filippova LV, Fedorova AV, Nozdrachev AD. Mechanism of Activation of Enteric Nociceptive Neurons via Interaction of TLR4 and TRPV1 Receptors. Dokl Biol Sci. 2018 Mar;479(1):44-46.
[5] Zhang SS, Liu M, Liu DN, et al. TLR4-IN-C34 Inhibits Lipopolysaccharide-Stimulated Inflammatory Responses via Downregulating TLR4/MyD88/NF-κB/NLRP3 Signaling Pathway and Reducing ROS Generation in BV2 Cells. Inflammation. 2022 Apr;45(2):838-850.
[6] Barbosa MLL, Costa DVDS, de Pacífico DM, et al. Role of TLR4 in Enteric Glia Response to Clostridioides Difficile Toxins: Insights From In Vivo and In Vitro Studies. J Cell Mol Med. 2025 Nov;29(22):e70943.
[7] Abdelsalam HM, Helal MG, Abu-Elsaad NM. TLR4-IN-C34 protects against acute kidney injury via modulating TLR4/MyD88/NF-κb axis, MAPK, and apoptosis. Iran J Basic Med Sci. 2022 Nov;25(11):1334-1340.
[8] Varmazyar R, Naderi N, Javid H, et al. Neuroprotective Effects of Early TLR4 Blockade with Compound C34 in Temporal Lobe Epilepsy: Alleviation of Neuroinflammation and Apoptosis. Iran J Pharm Res. 2025 Mar 8;24(1):e159165.
| Cell experiment [1]: | |
Cell lines | BV2 microglia cells (murine microglial cell line) |
Preparation Method | BV2 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were pretreated with C34 (10, 30, and 100μM) for 2 hours before exposure to LPS (200ng/mL) for 24 hours |
Reaction Conditions | 10–100μM; 2h pretreatment |
Applications | C34 significantly reduced LPS-induced production of pro-inflammatory factors (NO, TNF-α, IL-1β, IL-6, MCP-1) and suppressed the expression of iNOS and COX-2 at both mRNA and protein levels. C34 also inhibited the TLR4/MyD88/NF-κB signaling pathway by downregulating TLR4 and MyD88 expression, reducing NF-κB phosphorylation, and blocking NF-κB nuclear translocation. Additionally, TLR4-IN-C34 attenuated NLRP3 inflammasome activation (cleaved caspase-1, IL-1β, IL-18) and decreased intracellular ROS generation. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Rats were administered Lithium chloride (127mg/kg) 20 hours prior to, and Methylscopolamine (2mg/kg) 20 minutes before, the intraperitoneal injection of pilocarpine (40mg/kg) to induce status epilepticus (SE). C34 (1μg/rat) was administered intracerebroventricularly either 1 hour (early treatment) or 24 hours (late treatment) after Pilocarpine injection. Rats were sacrificed 48 hours post-SE for hippocampal tissue analysis. |
Dosage form | 1μg/rat; ICV; Single injection. |
Applications | Early C34 treatment (1 hour post-SE) significantly reduced neuronal death in hippocampal regions (CA1, CA2, CA3, CA4, DG), decreased mortality rate, and suppressed expression of neuroinflammatory (NF-κB, TNF-α) and apoptotic (caspase-3) markers. Late C34 treatment (24 hours post-SE) showed limited neuroprotective effects, highlighting the critical importance of early TLR4 inhibition in mitigating SE-induced damage. |
References: | |
| Cas No. | 40592-88-9 | SDF | |
| Synonyms | Toll-Like Receptor 4-C34 | ||
| Chemical Name | 3,4,6-triacetate-1-methylethyl 2-(acetylamino)-2-deoxy-α-D-glucopyranoside | ||
| Canonical SMILES | CC(C)O[C@H]1O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]1NC(C)=O | ||
| Formula | C17H27NO9 | M.Wt | 389.4 |
| Solubility | 50mg/mL in ethanol or in DMF, 25mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL |
| 5 mM | 513.6 μL | 2.5681 mL | 5.1361 mL |
| 10 mM | 256.8 μL | 1.284 mL | 2.5681 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)