TLR7/8 agonist 1 dihydrochloride |
Catalog No.GC30516 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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Purity: >98.00%
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Cell experiment: | Fresh human peripheral blood mononuclear cells (hPBMC) are used. 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]. |
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. |
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
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].
[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. [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.
Cas No. | 1620278-72-9 | SDF | |
Synonyms | N/A | ||
Chemical Name | N/A | ||
Canonical SMILES | NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3CC4=CC=C(CN)C=C4.[H]Cl.[H]Cl | ||
Formula | C22H27Cl2N5 | M.Wt | 432.39 |
Solubility | DMSO : 83.33 mg/mL (192.72 mM) | Storage | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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