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

TLR7-agonist-1 

Cat. No.: HY-103039 Purity: 98.82%
Handling Instructions

TLR7-agonist-1 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

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

TLR7-agonist-1 Chemical Structure

TLR7-agonist-1 Chemical Structure

CAS No. : 1642857-69-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 524 In-stock
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Estimated Time of Arrival: December 31
5 mg USD 708 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1068 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2148 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

In Vivo

TLR7-agonist-1 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-1 can induce an antiviral interferon stimulated gene (ISG) response without inducing an IFNα response at a low dose. TLR7-agonist-1 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].

Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (475.69 mM; Need ultrasonic and warming)

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
10 mM 0.2973 mL 1.4865 mL 2.9731 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

The ability of TLR7-agonist-1 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-1 is given to healthy, female, fasted C57Bl/6 mice. Concentrations of TLR7-agonist-1 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
Molecular Weight

336.35

Formula

C₁₇H₁₆N₆O₂

CAS No.

1642857-69-9

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TLR7-agonist-1
Cat. No.:
HY-103039
Quantity:

TLR7-agonist-1

Cat. No.: HY-103039