1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. CU-CPT22

CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM.

For research use only. We do not sell to patients.

CAS No. : 1416324-85-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of CU-CPT22:

Top Publications Citing Use of Products

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Anim Reprod Sci. 2024 May 31:266:107513.  [Abstract]

    Effect of TLR2 on the release of inflammatory mediators in EECs infected with LPS and E. coli in the presence of BLP. EECs were pretreated with the TLR2 inhibitor, CU-CPT22 (10  µM), before treatment for 4  h. EECs were treated with LPS (1  μg/mL) and BLP (1  μg/mL) in combination, or untreated (A-C). EECs were infected with JE5505 (1 × 106 CFU) in combination with BLP (1  μg/mL) or left uninfected (D-F). Release of IL-6, IL-8, and IL-10 into the supernatant of EECs cultures was analyzed by ELISA, 12  h after treatment.

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2020 May;241:119852.  [Abstract]

    The TLR2-MyD88-IKK-IκB-NF-κB signaling pathway was activated in DP7-C-stimulated BMDCs. Furthermore, Western blot results also showed that DP7-C failed to effectively activate MyD88 following treatment with TLR2 inhibitors (C29, CU-CPT22; 8 μM, 2 h), whereas DP7-C still activated MyD88 after treatment with the TLR4 inhibitor TAK242.

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Oral Dis. 2020;00:1-13.

    Representative H&E and F4/80 staining images of saline-injection, CFA-injection and CFA + CU-CPT22 (10 mg/kg; i.p.; administered once prior to TMJOA induction, and twice weekly thereafter) groups' synovium. In CFA-injection mice, the thickness of intimal layer at 2nd (b) and 4th (e) week was markedly higher than that in saline-injection mice (a, d); The intima layer thinned gradually in CTA + CU-CPT22 treated mice (c, f). Analogously, administration of CU-CPT22 (i) significantly inhibited the elevation of F4/80 positive staining in CFA-injection mice (h), compared with that of saline-injection mice (g), which displayed weak expression of F4/80 (Figure j stands for control with negative primary IgG).

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Oral Dis. 2020;00:1-13.

    The expression of anabolic factors aggrecan (ACAN) and type II collagen (Col2A1) at the 4th week was detected by immunofluorescence. In comparison with CFA-injection mice, CFA + CU-CPT22 (10 mg/kg; i.p.; administered once prior to TMJOA induction, and twice weekly thereafter) treated mice exhibited stronger and homogeneous positive expression of ACAN and Col2A1 on the condylar cartilage.

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Oral Dis. 2020;00:1-13.

    Immunoblots detection disclosed that pretreatment of CU-CPT22 (10 μM; pretreated 3 h) significantly reduced the production of TLR2, NF-κB p65, as well as catabolic factors (MMP3, MMP13) and inflammatory factors (TNF-α, COX-2) in chondrocytes induced by IL-1β (10 ng/mL).

    CU-CPT22 purchased from MedChemExpress. Usage Cited in: Life Sci. 2019 May 1:224:212-221.  [Abstract]

    WB for detecting the effect of CU-CPT22 (CU CPT, 0.58 μM; 1 h), an inhibitor of TLR2.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM[1].

    IC50 & Target

    TLR1

     

    TLR2

     

    In Vitro

    CU-CPT22 is a toll-like receptor 1 and 2 (TLR1/2) inhibitor with an IC50 of 0.58±0.09 μM. It is demonstrated that CU-CPT22 is able to compete with Pam3CSK4 for binding to TLR1/2 with an inhibition constant (Ki) of 0.41±0.07 μM, which is consistent with its potency observed in the whole cell assay. Increasing the concentration of CU-CPT22 to 6 μM decreases the anisotropy to background levels. It is found that CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. CU-CPT22 is found to have no significant cytotoxicity at various concentrations up to 100 μM in RAW 264.7 cells.? The result demonstrates that CU-CPT22 can inhibit about 60% of TNF-αand 95% of IL-1β at 8 μM[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    362.37

    Formula

    C19H22O7

    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(C(C=C1O)=CC2=CC(OC)=C(O)C(O)=C2C1=O)OCCCCCC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 125 mg/mL (344.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7596 mL 13.7981 mL 27.5961 mL
    5 mM 0.5519 mL 2.7596 mL 5.5192 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: ≥99.0%

    References
    Kinase Assay
    [1]

    RAW 264.7 cells are planted in 6-well plates at 1,000,000 cells per well with 3 mL of medium and grown for 24 h at 37°C in a 5% CO2 humidified incubator. After 24 h, non-adherent cells and media are removed and replaced with fresh RPMI 1640 medium (3 mL/well). Two wells of adherent macrophages are treated with Pam3CSK4 (300 ng/mL) as the positive control, two wells are treated with 8 μM CU-CPT22, and the other two wells are treated with 8 μM compound DMSO. Plates are then incubated for an additional 24 h. The medium is removed, the cells are washed with PBS (3×1 mL), the plate is put on ice, then 500 μL of lysis buffer is added to each well. The production of the cytokine interleukin-1β (IL-1β) and TNF-α is quantified with enzyme-linked immunosorbent assays (ELISA). The cytokine level in each sample is determined in duplicate[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7596 mL 13.7981 mL 27.5961 mL 68.9903 mL
    5 mM 0.5519 mL 2.7596 mL 5.5192 mL 13.7981 mL
    10 mM 0.2760 mL 1.3798 mL 2.7596 mL 6.8990 mL
    15 mM 0.1840 mL 0.9199 mL 1.8397 mL 4.5994 mL
    20 mM 0.1380 mL 0.6899 mL 1.3798 mL 3.4495 mL
    25 mM 0.1104 mL 0.5519 mL 1.1038 mL 2.7596 mL
    30 mM 0.0920 mL 0.4599 mL 0.9199 mL 2.2997 mL
    40 mM 0.0690 mL 0.3450 mL 0.6899 mL 1.7248 mL
    50 mM 0.0552 mL 0.2760 mL 0.5519 mL 1.3798 mL
    60 mM 0.0460 mL 0.2300 mL 0.4599 mL 1.1498 mL
    80 mM 0.0345 mL 0.1725 mL 0.3450 mL 0.8624 mL
    100 mM 0.0276 mL 0.1380 mL 0.2760 mL 0.6899 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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