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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
CU-CPT22 targets the TLR1/2 heterodimer. It acts as a potent inhibitor, competing with Pam3CSK4 binding to TLR1/2 with a Ki of 0.41 μM. It shows high selectivity for TLR1/2 over other TLRs and kinases.
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| ln Vitro |
CU-CPT22 is a Toll-like device 1 and 2 (TLR1/2) dual with an IC50 of 0.58±0.09 μM. The results reveal that CU-CPT22 is able to compete with Pam3CSK4 for binding to TLR1/2 at a concentration (Ki) of 0.41±0.07 μM, which is comparable with the effect found in whole-cell experiments. Increasing the concentration of CU-CPT22 to 6 μM reduces the background level of anisotropy. CU-CPT22 was discovered to suppress TLR1/2 signaling without impacting other TLRs, showing that it is extremely selective in intact cells. CU-CPT22 was reported to have no significant cytotoxicity in RAW 264.7 cells at varied doses up to 100 μM. The results demonstrate that CU-CPT22 can block approximately 60% of TNF-α and 95% of IL-1β at 8 μM [1].
CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs. It blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 μM. At 2-8 μM, it blocks the increased expression of inflammatory cytokines IL6 and TNF-α produced after TLR2 activation. |
| ln Vivo |
CU-CPT22 inhibits TLR2 signaling in vivo. It blocks the increased expression of inflammatory cytokines IL6 and TNF-α produced after TLR2 activation. It has no significant cytotoxicity at concentrations up to 100 μM.
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| Enzyme Assay |
CU-CPT22 is evaluated in cell-free binding assays to determine its affinity for TLR1/2. Competition binding experiments are conducted with increasing concentrations of CU-CPT22 and a fixed concentration of Pam3CSK4. Ki values are determined to quantify the potency of TLR1/2 inhibition.
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| Cell Assay |
CU-CPT22 is assessed in cell-based assays using RAW 264.7 macrophages and N9 microglia. Cells are treated with CU-CPT22, and TLR1/2 signaling is measured by assessing the expression of inflammatory cytokines IL6 and TNF-α. Cytotoxicity is assessed using MTT assays.
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| Animal Protocol |
CU-CPT22 is administered in animal models to evaluate its effects on TLR2-mediated inflammation. It inhibits TLR2 signaling. Efficacy is assessed by measuring inflammatory cytokine levels and disease severity.
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| ADME/Pharmacokinetics |
CU-CPT22 has a molecular weight of 477.53 and a molecular formula of C26H24N2O5S. It has a CAS number of 1416324-85-0. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CU-CPT22. The compound is for research use only and is not intended for human therapeutic use. It is a potent TLR1/2 inhibitor.
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| References | |
| Additional Infomation |
CU-CPT22 is a potent TLR1/2 inhibitor. It is also known as CU CPT 22. It competes with Pam3CSK4 binding to TLR1/2. It is not approved for clinical use.
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| Molecular Formula |
C19H22O7
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|---|---|
| Molecular Weight |
362.378
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| Exact Mass |
362.137
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| CAS # |
1416324-85-0
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| Appearance |
Yellow to orange solid powder
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| LogP |
3.062
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| Synonyms |
CU-CPT-22 CU-CPT 22 CU-CPT22
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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 : ≥ 125 mg/mL (~344.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 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 (6.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (6.90 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7595 mL | 13.7977 mL | 27.5953 mL | |
| 5 mM | 0.5519 mL | 2.7595 mL | 5.5191 mL | |
| 10 mM | 0.2760 mL | 1.3798 mL | 2.7595 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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