| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
CL097 activates NF-κB at 0.1 μM in TLR7-transfected HEK293 cells and at 4 μM in TLR8-transfected HEK293 cells [1]. By imitating the phosphorylation of p47phox in the human neutrophil signaling system, CL097 causes overactivation of NADPH oxidase, suggesting that p38 MAPK, ERK1/2, protein inhibitor C, and Pin1 regulate this process. CL097 increases fmlf-induced p47phox and causes phosphorylation of p47phox at particular locations.
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|---|---|
| ln Vivo |
CL097 and CD40 agonists promote significant diabetogenic cytotoxic T pathway (CTL) activity in NOD mice. CL097 (5 mg/kg, sc) alone induced possible excess (~25%) of the target peptide. However, combination treatment with CL097 and a CD40 agonist (10 mg/kg, ip) resulted in an approximately twofold increase in the oscillation frequency of IGRP peptide-coated targets compared to treatment with CL097 alone [3].
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| Cell Assay |
Western Blot analysis [2]
Cell Types: Neutrophil Tested Concentrations: 0, 0.5, 2.5, 5 and 10 μg/mL Incubation Duration: 30 minutes of pretreatment Experimental Results: Induces phosphorylation of p47phox at specific sites at a certain concentration [2]. Dependence method. |
| Animal Protocol |
Animal/Disease Models: Female 8.3 NOD mice (5-6 weeks old) [3]
Doses: 5 mg/kg Route of Administration: subcutaneous injection Experimental Results: Caused moderate specific cleavage of the target peptide (∼25%). |
| References |
[1]. Cindy Patinote, et al. Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes. Eur J Med Chem. 2020 May 1;193:112238.
[2]. Karama Makni-Maalej, et al. The TLR7/8 agonist CL097 primes N-formyl-methionyl-leucyl-phenylalanine-stimulated NADPH oxidase activation in human neutrophils: critical role of p47phox phosphorylation and the proline isomerase Pin1. J Immunol. 2012 Nov 1;189(9):4657-65. [3]. A S Lee, et al. Toll-like receptor 7 stimulation promotes autoimmune diabetes in the NOD mouse. Diabetologia. 2011 Jun;54(6):1407-16. |
| Molecular Formula |
C13H14N4O
|
|---|---|
| Molecular Weight |
242.28
|
| CAS # |
1026249-18-2
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| Related CAS # |
CL097 hydrochloride
|
| SMILES |
N1C2C(=CC=CC=2)C2N=C(COCC)NC=2C=1N
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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 : ~100 mg/mL (~412.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.32 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 (10.32 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1275 mL | 20.6373 mL | 41.2746 mL | |
| 5 mM | 0.8255 mL | 4.1275 mL | 8.2549 mL | |
| 10 mM | 0.4127 mL | 2.0637 mL | 4.1275 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.
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