TLR7/8/9-IN-1
Based on 2 publication(s) in Google Scholar
TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
For research use only. We do not sell to patients.
- Purity: 98.51%
- CAS No.: 2180127-82-4
- Formula: C27H37N3O2
- Molecular Weight:435.60
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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) TLR7/8/9-IN-1
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Customer Validation & Images
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Cell Imaging/Staining
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>50000 nM
Compound: 7f
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Agonist activity at human TLR8 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay
Agonist activity at human TLR8 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay
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[PMID: 32944143] |
| HEK293 | IC50 |
>50000 nM
Compound: 7f
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Agonist activity at human TLR7 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay
Agonist activity at human TLR7 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay
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[PMID: 32944143] |
| PBMC | IC50 |
4.8 nM
Compound: 7f
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Antagonist activity at TLR7 (unknown origin) in PBMC cells assessed as reduction of IL-6 production
Antagonist activity at TLR7 (unknown origin) in PBMC cells assessed as reduction of IL-6 production
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[PMID: 32944143] |
| PBMC | IC50 |
510 nM
Compound: 7f
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Antagonist activity at TLR9 (unknown origin) in PBMC cells assessed as reduction of IL-6 production
Antagonist activity at TLR9 (unknown origin) in PBMC cells assessed as reduction of IL-6 production
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[PMID: 32944143] |
Chemical Information
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CAS No. 2180127-82-4
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Appearance Solid
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Molecular Weight 435.60
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Formula C27H37N3O2
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Color Off-white to light yellow
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SMILES
CNCCN1CCC(C2=CC3=C(NC(C4=CC=C(OC)C(OC)=C4)=C3C(C)C)C=C2)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Neutrophil extracellular traps induced by the hypoxic microenvironment in gastric cancer augment tumour growth. [Abstract]2023 May 1;21(1):86. PMID: 37127629
TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the p-p38 level in neutrophils was measured by western blotting.
TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the NET formation was detected with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm. All values are the means ± SDs. ns = not significant, **P < 0.01
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Adv Biol (Weinh)
HMGB1 Derived from the Pyroptotic Microenvironment Promotes Macrophage Extracellular Traps in Hirschsprung-Associated Enterocolitis. [Abstract]2025 Sep;9(9):e00761. PMID: 40464207
TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Sep;9(9):e00761. [Abstract]
Macrophages were pretreated with inhibitors of TLR2 (MMG-11; HY‐112146), TLR4 (Resatorvid; HY‐11109), TLR9 (TLR7/8/9-IN-1; HY-131952) and RAGE (RAGE antagonist peptide; HY‐P2268) prior to coculture with pyroptotic‐CM, and the p‐p38 and p‐p65 levels in macrophages were measured by western blotting.
Solvent & Solubility
DMSO : 83.33 mg/mL (191.30 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.78 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.78 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 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 | 2.2957 mL | 11.4784 mL | 22.9568 mL | 57.3921 mL |
| 5 mM | 0.4591 mL | 2.2957 mL | 4.5914 mL | 11.4784 mL | |
| 10 mM | 0.2296 mL | 1.1478 mL | 2.2957 mL | 5.7392 mL | |
| 15 mM | 0.1530 mL | 0.7652 mL | 1.5305 mL | 3.8261 mL | |
| 20 mM | 0.1148 mL | 0.5739 mL | 1.1478 mL | 2.8696 mL | |
| 25 mM | 0.0918 mL | 0.4591 mL | 0.9183 mL | 2.2957 mL | |
| 30 mM | 0.0765 mL | 0.3826 mL | 0.7652 mL | 1.9131 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5739 mL | 1.4348 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4591 mL | 1.1478 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3826 mL | 0.9565 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7174 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5739 mL |
TLR7/8/9-IN-1 Related Classifications
HY-131952 Related Classifications
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