TLR7/8 agonist 1

Name: TLR7/8 agonist 1
Brand: MedChemExpress
SKU: HY-103698
Rating: 4.5 (1 reviews)

Cat. No.: HY-103698 Purity: 97.33%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

TLR7/8 agonist 1 Chemical Structure

CAS No. : 1258457-59-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 157	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 157	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 143	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 231	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1375	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of TLR7/8 agonist 1:

TLR7/8 agonist 1 dihydrochloride In-stock

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Protocol
Purity & Documentation
References
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Description

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

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.

Molecular Weight

359.47

Formula

C₂₂H₂₅N₅

CAS No.

1258457-59-8

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
10 mM	0.2782 mL	1.3909 mL	2.7819 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 97.33%

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Data Sheet (276 KB) SDS (251 KB)

COA (249 KB) HNMR (135 KB) LCMS (102 KB)

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]

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	[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

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

TLR7/8 agonist 1 Related Classifications

Inflammation/Immunology

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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TLR7/8 agonist 1

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Complete Stock Solution Preparation Table

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