Art. -Nr.: HY-131945

CU-115

2 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.63%
CAS. Nr.: 2471982-20-2
Formel: C₂₁H₁₁F₇INO₂
Molecular Weight:569.21

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CU-115 Chemical Structure

CAS. Nr.: 2471982-20-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1].

IC₅₀ & Target^[1]

TLR8

1.04 μM (IC₅₀)

TLR7

50 μM (IC₅₀)

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>50 μM Compound: 14f; CU-115	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	[PMID: 31687820]
HEK293	IC₅₀	1.04 μM Compound: 14f; CU-115	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	[PMID: 31687820]

In Vitro

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

CAS. Nr. 2471982-20-2
Appearance Solid
Molecular Weight 569.21
Formel C₂₁H₁₁F₇INO₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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ACS Nano

Separable Microneedle Patch to Protect and Deliver DNA Nanovaccines Against COVID-19. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7568 mL

8.7841 mL

17.5682 mL

5 mM

0.3514 mL

1.7568 mL

3.5136 mL

10 mM

0.1757 mL

0.8784 mL

1.7568 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Rosaura Padilla-Salinas, et al. Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors 7 and 8. J Med Chem. 2019 Nov 27;62(22):10221-10244. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CU-115

2 Cited Publications

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CU-115

Immunology/Inflammation Compound Library

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Antioxidant Compound Library

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Pyroptosis Compound Library

Antidepressant Compound Library

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Pain-Related Compound Library

Membrane Protein-targeted Compound Library

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Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) CU-115

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CU-115

Immunology/Inflammation Compound Library

Small Molecule Immuno-Oncology Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Antidepressant Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Publications Citing Use of MedChemExpress (MCE) CU-115

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CU-115 Related Classifications

Art. -Nr.: HY-131945