1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. CU-T12-9

CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

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CU-T12-9 Chemical Structure

CU-T12-9 Chemical Structure

CAS No. : 1821387-73-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
1 mg USD 133 In-stock
5 mg USD 280 In-stock
10 mg USD 360 In-stock
50 mg USD 550 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].

IC50 & Target[1]

TLR2

52.9 nM (EC50, in HEK-Blue cells)

TLR1

52.9 nM (EC50, in HEK-Blue cells)

In Vitro

CU-T12-9 directly targets TLR1/2 to initiate downstream signaling. By binding to both TLR1 and TLR2, CU-T12-9 facilitates the TLR1/2 heterodimeric complex formation, which in turn activates the downstream signaling[1].
CU-T12-9 activates the TLR1/2 pathway by inducing NF-κB activation to trigger downstream signaling, such as secreted embryonic alkaline phosphatase (SEAP), NO, and TNF-α[1].
CU-T12-9 (0.39-100 μM; 24 hours) does not produce toxicity up to 100 μM in HEK-Blue hTLR2 and Raw 264.7 cells[1].
CU-T12-9 up-regulates the mRNA levels of TLR1, TLR2, TNF, IL-10, and iNOS. CU-T12-9 (0.1-10 μM) activates TLR1 mRNA and iNOS mRNA after Raw 264.7 cells are treated for 24 hours. CU-T12-9 (0.1-10 μM) activates TLR2 and IL-10 mRNA after Raw 264.7 cells are treated for 2 hours. CU-T12-9 (0.1-10 μM) activates TNF mRNA after Raw 264.7 cells are treated for 8 hours[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HEK-Blue hTLR2 and Raw 264.7 macrophage cells
Concentration: 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50, and 100 μM
Incubation Time: 24 hours
Result: No toxicity was seen up to 100 μM.

RT-PCR[1]

Cell Line: Raw 264.7 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 hours for TLR1 and iNOS mRNA assay
2 hours for TLR2 and IL-10 mRNA assay
8 hours for TNF mRNA assay
Result: Triggered TLR1 mRNA and iNOS mRNA at 24 hours dose-dependently.
Dose-dependent activation of TLR2 mRNA and IL-10 mRNA at 2 hours.
Showed dose-dependent activation of TNF mRNA at 8 hours.
Molecular Weight

362.31

Formula

C17H13F3N4O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CNC1=CC=C(C=C1N2C=C(N=C2)C3=CC=C(C=C3)C(F)(F)F)[N+]([O-])=O

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 : 250 mg/mL (690.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7601 mL 13.8003 mL 27.6007 mL
5 mM 0.5520 mL 2.7601 mL 5.5201 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: ≥ 2.08 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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: 98.94%

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 2.7601 mL 13.8003 mL 27.6007 mL 69.0017 mL
5 mM 0.5520 mL 2.7601 mL 5.5201 mL 13.8003 mL
10 mM 0.2760 mL 1.3800 mL 2.7601 mL 6.9002 mL
15 mM 0.1840 mL 0.9200 mL 1.8400 mL 4.6001 mL
20 mM 0.1380 mL 0.6900 mL 1.3800 mL 3.4501 mL
25 mM 0.1104 mL 0.5520 mL 1.1040 mL 2.7601 mL
30 mM 0.0920 mL 0.4600 mL 0.9200 mL 2.3001 mL
40 mM 0.0690 mL 0.3450 mL 0.6900 mL 1.7250 mL
50 mM 0.0552 mL 0.2760 mL 0.5520 mL 1.3800 mL
60 mM 0.0460 mL 0.2300 mL 0.4600 mL 1.1500 mL
80 mM 0.0345 mL 0.1725 mL 0.3450 mL 0.8625 mL
100 mM 0.0276 mL 0.1380 mL 0.2760 mL 0.6900 mL
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CU-T12-9 Related Classifications

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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CU-T12-9
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