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Purity: ≥98%
TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling. It is induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.
ln Vitro |
In HEK-TLR2 stable transfectants, C29 (10 or 50 μM; 1 hour) suppresses IL-8 mRNA produced by P3C and P2C in a dose-inducible manner. Significant inhibition of P3C- and P2C-induced IL-1β gene expression occurs at 1 and 4 hours following THP-1 cell stimulation with C29 (50 - 200 μM; 1 hour) [1]. Oxygen agonist Induced pro-inflammatory gene expression[1] by TNF-α mRNA[1] and IL-12 p40 protein[1]; C29 (50 μM; 1 hour) suppresses TLR2 in HEK-TLR2 cells and mouse macrophages; and C29 (25 or 50 μM; 1 hour) greatly lowers P3C sensing diode P2C sensing in primary mouse macrophages.
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Cell Assay |
Western Blot Analysis [1]
Cell Types: THP-1 Cell Tested Concentrations: 150 μM Incubation Duration: 1 hour Experimental Results: Interaction between endogenous TLR2 and myeloid differentiation primary response gene 88 (MyD88) 15 and 30 minutes after stimulation with P3C The effect is weakened. Western Blot Analysis [1] Cell Types: Murine peritoneal macrophages Tested Concentrations: 50 μM Incubation Duration: 1 hour Experimental Results: Strong blockade of MAPK activation at 30 minutes and diminished NF-κB activation from 5 to 30 minutes. Prevents P3C-induced IκBα degradation at 15 and 30 min. |
References |
[1]. Mistry P, 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 Apr 28;112(17):5455-60.
[2]. Cai S, Zhu G, Cen X, et al. Synthesis, structure-activity relationships and preliminary mechanism study of N-benzylideneaniline derivatives as potential TLR2 inhibitors. Bioorg Med Chem. 2018;26(8):2041-2050. |
Molecular Formula |
C16H15NO4
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Molecular Weight |
285.29
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Exact Mass |
285.1001
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Elemental Analysis |
C, 67.36; H, 5.30; N, 4.91; O, 22.43
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CAS # |
363600-92-4
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Related CAS # |
363600-92-4;
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Appearance |
Solid powder
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SMILES |
O=C(O)C1=CC=CC(/N=C/C2=CC=CC(OC)=C2O)=C1C
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InChi Key |
WTGMGRFVBFDHGQ-RQZCQDPDSA-N
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InChi Code |
InChI=1S/C16H15NO4/c1-10-12(16(19)20)6-4-7-13(10)17-9-11-5-3-8-14(21-2)15(11)18/h3-9,18H,1-2H3,(H,19,20)/b17-9+
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Chemical Name |
3-[[(2-Hydroxy-3-methoxyphenyl)methylene]amino]-2-methyl-benzoic acid
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Synonyms |
TLR2-IN-C29 TLR2 IN C29 TLR2INC29 TLR2-inhibitor-C29 TLR2 inhibitor-C29 TLR2 inhibitor C29
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~105.16 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5052 mL | 17.5260 mL | 35.0521 mL | |
5 mM | 0.7010 mL | 3.5052 mL | 7.0104 mL | |
10 mM | 0.3505 mL | 1.7526 mL | 3.5052 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.