TLR7/8 agonist 1
Based on 1 publication(s) in Google Scholar
TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
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- Reinheit: 98.42%
- CAS. Nr.: 1258457-59-8
- Formel: C22H25N5
- Molecular Weight:359.47
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TLR7/8 agonist 1
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Biologische Aktivität
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TLR7 |
TLR8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
528 nM
Compound: 1
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Agonist activity at human TLR7 transfected in HEK reporter cells assessed as NF-kappaB induction by specific secreted alkaline phosphatase gene assay
Agonist activity at human TLR7 transfected in HEK reporter cells assessed as NF-kappaB induction by specific secreted alkaline phosphatase gene assay
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[PMID: 21549593] |
| HEK293 | EC50 |
55 nM
Compound: 1
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Agonist activity at human TLR8 transfected in HEK293 cells assessed as activation of NF-kB by reporter gene assay
Agonist activity at human TLR8 transfected in HEK293 cells assessed as activation of NF-kB by reporter gene assay
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[PMID: 26351878] |
TLR7/8 agonist 1 (Compound 5d) shows prominent immunostimulatory activities. TLR7/8 agonist 1 serves as a convenient precursor for the covalent attachment of fluorophores without significant loss of activity.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM. TLR7/8 agonist 1 is covalently coupled directly to commercially-available fluorescein isothiocyanate and rhodamine B isothiocyanate[1]. TLR7/8 agonist 1 (Compound 1) shows substantially different agonistic potencies in human TLR7 (50 nM) and TLR8 (55 nM) primary screens[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1258457-59-8
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Appearance Solid
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Molecular Weight 359.47
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Formel C22H25N5
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Color Off-white to light yellow
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SMILES
NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3CC4=CC=C(CN)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Gut
2025 Nov 12:gutjnl-2025-335806. PMID: 41198172
Lösungsmittel & Löslichkeit
DMSO : 11.11 mg/mL (30.91 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
The induction of NF-κB is quantified using human TLR-2, TLR3, TLR4, TLR5, TLR7, TLR8, TLR9, and NOD-1/NOD-2-specific, rapid-throughput, liquid handler-assisted reporter gene assays. HEK293 cells stably co-transfected with the appropriate hTLR (or NOD) and secreted alkaline phosphatase (sAP) are maintained in HEK-Blue Selection medium. Stable expression of secreted alkaline phosphatase (sAP) under control of NF-κB/AP-1 promoters is inducible by appropriate TLR/NOD agonists, and extracellular sAP in the supernatant is proportional to NF-κB induction. Reporter cells are incubated at a density of ~105 cells/mL in a volume of 80 μL/well, in 384-well, flat-bottomed, cell culture-treated microtiter plates in the presence of graded concentrations of stimuli. sAP is assayed spectrophotometrically using an alkaline phosphatase-specific chromogen (present in HEK-detection medium) at 620 nm[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fresh human peripheral blood mononuclear cells (hPBMC) are isolated from human blood obtained by venipuncture with informed consent and as per institutional guidelines on Ficoll–Hypaque gradients. Aliquots of PBMCs (105 cells in 100 μL/well) are stimulated for 12 h with graded concentrations of test compounds (e.g., TLR7/8 agonist 1; 0.1, 1, 10, and 100 μg/mL). Supernatants are isolated by centrifugation and are assayed in duplicates using analyte-specific multiplexed cytokine/chemokine bead array assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Shukla NM, et al. Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6384-6. [Content Brief]
[2]. Beesu M, et al. Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity. J Med Chem. 2015 Oct 8;58(19):7833-49. [Content Brief]
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 | 2.7819 mL | 13.9094 mL | 27.8187 mL | 69.5468 mL |
| 5 mM | 0.5564 mL | 2.7819 mL | 5.5637 mL | 13.9094 mL | |
| 10 mM | 0.2782 mL | 1.3909 mL | 2.7819 mL | 6.9547 mL | |
| 15 mM | 0.1855 mL | 0.9273 mL | 1.8546 mL | 4.6365 mL | |
| 20 mM | 0.1391 mL | 0.6955 mL | 1.3909 mL | 3.4773 mL | |
| 25 mM | 0.1113 mL | 0.5564 mL | 1.1127 mL | 2.7819 mL | |
| 30 mM | 0.0927 mL | 0.4636 mL | 0.9273 mL | 2.3182 mL |
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