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TLR7/8 agonist 1 dihydrochloride

Catalog No.GC30516

A dual agonist of TLR7 and TLR8

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TLR7/8 agonist 1 dihydrochloride Chemical Structure

Cas No.: 1620278-72-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$297.00
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5mg
$270.00
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10mg
$441.00
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25mg
$864.00
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50mg
$1,305.00
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100mg
$2,122.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.
[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.

Background

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.

Chemical Properties

Cas No. 1620278-72-9 SDF
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 Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3127 mL 11.5636 mL 23.1273 mL
5 mM 0.4625 mL 2.3127 mL 4.6255 mL
10 mM 0.2313 mL 1.1564 mL 2.3127 mL
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for TLR7/8 agonist 1 dihydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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