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

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

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TLR7 agonist 2 Chemical Structure

TLR7 agonist 2 Chemical Structure

CAS No. : 1642857-69-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 466 In-stock
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10 mM * 1 mL in DMSO USD 466 In-stock
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1 mg USD 195 In-stock
5 mg USD 630 In-stock
10 mg USD 910 In-stock
50 mg USD 2730 In-stock
100 mg USD 4000 In-stock
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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TLR7 agonist 2

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Description

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

IC50 & Target

LEC: 0.4 μM (TLR7)[1]

In Vitro

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a lowest effective concentration (LEC) of 0.4 μM in HEK293 cell. TLR7 agonist 2 is found to be selective for TLR7 over TLR8 with LEC of >100 μM for human TLR8. TLR7 agonist 2 demonstrates low inhibition across five CYP450 isozymes (IC50 >10 μM) and is also not a time dependent inhibitor of CYP450 3A4. TLR7 agonist 2 has limited inhibition of the hERG potassium ion channel 3H-dofetilide binding in vitro (IC50 >50 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TLR7 agonist 2 is found to be rapidly cleared in conjunction with our target profile. Both Cmax and AUC increase less than dose proportionally between 0.3 and 3 mg/kg and more than dose-proportionally between 3 and 10 mg/kg. TLR7 agonist 2 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7 agonist 2 also induces a 2.7 log decrease in serum HBV viral load from 0.3 mg/kg, and a maximum 3.1 log decrease is observed for doses between 1 and 5 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

336.35

Formula

C17H16N6O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(COC2=C(N(CC3=NC=CC=C3)C=C4)C4=NC(N)=N2)=NO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (475.69 mM; Need ultrasonic and warming; 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 2.9731 mL 14.8655 mL 29.7309 mL
5 mM 0.5946 mL 2.9731 mL 5.9462 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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
References
Cell Assay
[1]

The ability of TLR7 agonist 2 to activate human TLR7 and/or TLR8 is assessed by using HEK293 cells. Briefly, HEK293 cells are grown in culture medium (DMEM supplemented with 10% FCS and 2 mM Glutamine). Transfected cells are then detached with Trypsin-EDTA, washed in PBS and resuspended in medium to a density of 1.67×105 cells/mL. Thirty microliters of cells are then dispensed into each well in 384-well plates, where 10 μL of TLR7-agonist-1 in 4% DMSO is already present. Following 6 hours incubation at 37°C, 5% CO2, the luciferase activity is determined by adding 15 μL of Steady Lite Plus substrate to each well and readout performed on a microplate imager. Lowest effective concentrations (LEC) values are determined for TLR7-agonist-1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

A mouse in vivo model is used to demonstrate the initial proof of concept to induce endogenous IFNα. Single oral administration of 0.3, 1, 3, and 10 mg/kg doses of TLR7 agonist 2 is given to healthy, female, fasted C57Bl/6 mice. Concentrations of TLR7 agonist 2 and mouse-IFN via ELISA are measured from the plasma and compare to vehicle[1].

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9731 mL 14.8655 mL 29.7309 mL 74.3273 mL
5 mM 0.5946 mL 2.9731 mL 5.9462 mL 14.8655 mL
10 mM 0.2973 mL 1.4865 mL 2.9731 mL 7.4327 mL
15 mM 0.1982 mL 0.9910 mL 1.9821 mL 4.9552 mL
20 mM 0.1487 mL 0.7433 mL 1.4865 mL 3.7164 mL
25 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9731 mL
30 mM 0.0991 mL 0.4955 mL 0.9910 mL 2.4776 mL
40 mM 0.0743 mL 0.3716 mL 0.7433 mL 1.8582 mL
50 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
60 mM 0.0496 mL 0.2478 mL 0.4955 mL 1.2388 mL
80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9291 mL
100 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7433 mL
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TLR7 agonist 2 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.

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TLR7 agonist 2
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