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.
For research use only. We do not sell to patients.
- Purity : 98.42%
- CAS No.: 1258457-59-8
- Formula: C22H25N5
- Molecular Weight:359.47
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) TLR7/8 agonist 1
More
Biological Activity
Description
IC50 & Target
|
TLR7 |
TLR8 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
528 nM
Compound: 1
|
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
|
[PMID: 21549593] |
| HEK293 | EC50 |
55 nM
Compound: 1
|
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
|
[PMID: 26351878] |
In Vitro
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 No. 1258457-59-8
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Appearance Solid
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Molecular Weight 359.47
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Formula 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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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 (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
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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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)
References
[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 |