2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. TLR7/8 agonist 1

TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

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TLR7/8 agonist 1 Chemical Structure

TLR7/8 agonist 1 Chemical Structure

CAS No. : 1258457-59-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of TLR7/8 agonist 1:

TLR7/8 agonist 1 Related Antibodies

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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Description

TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

IC50 & Target

TLR7

 

TLR8

 

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.

TLR7/8 agonist 1 Related Antibodies
Molecular Weight

359.47

Formula

C22H25N5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3CC4=CC=C(CN)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7819 mL 13.9094 mL 27.8187 mL
5 mM 0.5564 mL 2.7819 mL 5.5637 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References
Kinase Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.7819 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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TLR7/8 agonist 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TLR7/8 agonist 11258457-59-8Toll-like Receptor (TLR)Inhibitorinhibitorinhibit

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