CU-115
Based on 2 publication(s) in Google Scholar
CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 2471982-20-2
- Formula: C21H11F7INO2
- Molecular Weight:569.21
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CU-115
More
Biological Activity
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TLR8 1.04 μM (IC50) |
TLR7 50 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>50 μM
Compound: 14f; CU-115
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Inhibition of human TLR7 expressed in HEK293 cells assessed as reduction in R848-induced NFkappaB production incubated for 16 hrs by quanti-blue SEAP assay
Inhibition of human TLR7 expressed in HEK293 cells assessed as reduction in R848-induced NFkappaB production incubated for 16 hrs by quanti-blue SEAP assay
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[PMID: 31687820] |
| HEK293 | IC50 |
1.04 μM
Compound: 14f; CU-115
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Inhibition of human TLR8 expressed in HEK293 cells assessed as reduction in R848-induced NFkappaB production incubated for 16 hrs by quanti-blue SEAP assay
Inhibition of human TLR8 expressed in HEK293 cells assessed as reduction in R848-induced NFkappaB production incubated for 16 hrs by quanti-blue SEAP assay
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[PMID: 31687820] |
In endosomal and non-endosomal TLR specificity studies, Human embryonic kidney (HEK) 293 cells expressing human tolllike receptor (hTLR) gene and an inducible secreted embryonic alkaline phosphatase (SEAP) reporter gene were incubated with CU-115 for 16 hours. As a result, CU-115 displays activity for TLR7 and TLR8 at low concentrations (0.5 μM).CU-115 does not modulate the NF-kB inhibition induced by Pam2CSK4, Pam3CSK4, Poly(I:C), LPS, R848, and Flic in HEK-293 TLR1/2, TLR2/6, TLR3, and TLR4 cells. And CU-115 inhibits TLR9 signaling at 1, 5, and 20 µM and ~10-25% inhibition.CU-115 (5-20 µM) inhibits increases in type I IFN transcriptional activity induced by the ssRNA nucleic acid ligands 3p-hpRNA or G3-YSD in a luciferase reporter assay.CU-115 (0.5, 1.0, 5, and 20 µM; 16 hours) is nontoxic at low concentrations (0.5 and 20 μM) and toxic at 100 μM in Hek293 TLR7 and TLR8 cells. CU-115 also is nontoxic at low concentrations (0.5 and 20 μM) and displays partial toxicity at 100 μM in THP Dual cells.The enzyme-linked immunosorbent assay (ELISA) is performed to measure upregulation/inhibition of TNF-α in human THP-1 cells (hTHP-1). CU-115 (5-20 µM) abolishes the TNF-α production activated by R848 (1 µg/ml) in hTHP1. It also represses the expression of IL-1β in hTHP-1 cells. These results suggest that CU-115 suppresses TLR8 and TLR7 signaling pathways.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2471982-20-2
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Appearance Solid
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Molecular Weight 569.21
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Formula C21H11F7INO2
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C=C1)C3=C(I)C=CC=C3F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Nano
2021 Sep 28;15(9):14347-14359. PMID: 34472328 -
Int J Mol Sci
CXCL4-RNA Complexes Circulate in Systemic Sclerosis and Amplify Inflammatory/Pro-Fibrotic Responses by Myeloid Dendritic Cells. [Abstract]2022 Dec 30;24(1):653. PMID: 36614095
Solvent & Solubility
DMSO : 100 mg/mL (175.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7568 mL | 8.7841 mL | 17.5682 mL | 43.9205 mL |
| 5 mM | 0.3514 mL | 1.7568 mL | 3.5136 mL | 8.7841 mL | |
| 10 mM | 0.1757 mL | 0.8784 mL | 1.7568 mL | 4.3921 mL | |
| 15 mM | 0.1171 mL | 0.5856 mL | 1.1712 mL | 2.9280 mL | |
| 20 mM | 0.0878 mL | 0.4392 mL | 0.8784 mL | 2.1960 mL | |
| 25 mM | 0.0703 mL | 0.3514 mL | 0.7027 mL | 1.7568 mL | |
| 30 mM | 0.0586 mL | 0.2928 mL | 0.5856 mL | 1.4640 mL | |
| 40 mM | 0.0439 mL | 0.2196 mL | 0.4392 mL | 1.0980 mL | |
| 50 mM | 0.0351 mL | 0.1757 mL | 0.3514 mL | 0.8784 mL | |
| 60 mM | 0.0293 mL | 0.1464 mL | 0.2928 mL | 0.7320 mL | |
| 80 mM | 0.0220 mL | 0.1098 mL | 0.2196 mL | 0.5490 mL | |
| 100 mM | 0.0176 mL | 0.0878 mL | 0.1757 mL | 0.4392 mL |
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