C29 (Synonyms: TLR2-IN-C29) |
Catalog No.GC33820
One-Click Copy Product Info
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C29 is a Toll-like receptor 2 (TLR2) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 363600-92-4
Sample solution is provided at 25 µL, 10mM.
C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29, inhibited TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages. C29 failed to inhibit signaling induced by other TLR agonists and TNF-α. Mutagenesis of BB loop pocket residues revealed an indispensable role for TLR2/1, but not TLR2/6, signaling, suggesting divergent roles [1].
C29 inhibited TLR2/1-mediated NF-κB activation (IC50 0.87µM), and inhibited TLR2/6 heterodimer with IC50 23µM [2]. C29 and o-vanillin may function by specifically targeting the BB loop pocket of the TLR2 TIR domain, altering its function and/or position [1].
Mice were pretreated with C29 before the administration of hepatitis B e antigen (HBeAg), to verify the roles of TLR-2 in vivo, the expression of IL-6, TNF-α, and CCL-2 was significantly alleviated, but IL-10 was upregulated in the liver [3]. C29 did not affect lipid accumulation, but the adipogenesis inhibitory effects of exopolysaccharide (EPS) significantly decreased in the C29-treated group. The results showed that activation of the AMPK signalling pathway by EPS was inhibited in the early stage (day 4) of adipogenic differentiation, when TLR2 and myeloid differentiation primary response 88 (MyD88) expression is inhibited by C29, indicating that EPS activates the AMPK signalling pathway by interacting with TLR2, consequently inhibiting adipogenesis [4].
References:
[1]. Mistry P, Laird MH, Schwarz RS, Greene S, Dyson T, Snyder GA, et al. Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain. Proc Natl Acad Sci U S A (2015) 112(17):5455-60. doi:10.1073/pnas.1422576112
[2]. Grabowski, M.; Murgueitio, M.S.; Bermudez, M.; Wolber, G.; Weindl, G. The novel small-molecule antagonist MMG-11 preferentially inhibits TLR2/1 signaling. Biochem. Pharmacol. 2020, 171, 113687.
[3]. Xie X, Lv H, Liu C, Su X, Yu Z, Song S, et al. HBeAg Mediates Inflammatory Functions of Macrophages by TLR2 Contributing to Hepatic Fibrosis. BMC Med (2021) 19:247. doi: 10.1186/s12916-021-02085-3
[4]. Lee, J.; Park, S.; Oh, N.; Park, J.; Kwon, M.; Seo, J.; Roh, S. Oral intake of Lactobacillus plantarum L-14 extract alleviates TLR2-and AMPK-mediated obesity- associated disorders in hight-fat-diet-induced obese C57BL/6J mice. Cell Prolif. 2021, 54, e13039
| Cell experiment [1]: | |
Cell lines | HEK-Blue cells,RAW macrophages,THP-1 macrophages |
Preparation Method | C29 were dissolved in DMSO as 50mM stock solution. Final DMSO concentrations in cell culture were below 0.2% (v/v). The cells were first incubated with the C29 for 1h and afterwards stimulated with the respective TLR(Toll like receptor) agonist. |
Reaction Conditions | 0.01µM, 0.1µM, 1µM, 10µM 100µM for 1 hour |
Applications | C29 showed inhibit affection for TLR2/1 or TLR2/6 (IC50 21µM and 23µM). |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | C29 was dissolved and diluted in solution (10% DMSO/40% PEG300/5% Tween-80/45% saline), then injected intraperitoneally (1.3 µmol/g) 1 h before HBeAg treatment, with the same volume of dissolving reagent as the vehicle group. |
Dosage form | Intraperitoneal injection, 1.3 µmol/g |
Applications | To verify the roles of TLR-2 in vivo, mice were pretreated with C29 before the administration of HBeAg. The expression of IL-6, TNF-α, and CCL-2 was significantly alleviated, but IL-10 was upregulated in the liver. |
References: | |
| Cas No. | 363600-92-4 | SDF | |
| Synonyms | TLR2-IN-C29 | ||
| Canonical SMILES | OC1=C(/C=N/C2=C(C)C(C(O)=O)=CC=C2)C=CC=C1OC | ||
| Formula | C16H15NO4 | M.Wt | 285.29 |
| Solubility | DMSO : ≥ 30 mg/mL (105.16 mM) | 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 | 3.5052 mL | 17.526 mL | 35.0521 mL |
| 5 mM | 701 μL | 3.5052 mL | 7.0104 mL |
| 10 mM | 350.5 μL | 1.7526 mL | 3.5052 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)