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

TLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice.

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TLR7 agonist 1

TLR7 agonist 1 Chemical Structure

CAS No. : 2178156-33-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

TLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice[1].

IC50 & Target[1]

TLR7

 

Cellular Effect
Cell Line Type Value Description References
HEK293 CC50
> 25 μM
Compound: 48
Cytotoxic activity against HEK293 cells assessed as reduction in cell viability incubated for 6 hrs
Cytotoxic activity against HEK293 cells assessed as reduction in cell viability incubated for 6 hrs
[PMID: 29366653]
In Vitro

TLR7 agonist 1 (compound 48) (0.09 μM) is a highly potent, TLR7-selective agonist (SI >200 over TLR8) in HEK-293 cells transiently transfected with human TLR7, with an hTLR7 LEC of 0.09 μM[1].
TLR7 agonist 1 (0.14 μM) induces IFN-α in hPBMCs with an LEC50 of 0.14 μM[1].
TLR7 agonist 1 (>25 μM) has low cytotoxicity in HEK-293 cells[1].
TLR7 agonist 1 (1 μM; 15 min) exhibits moderate metabolic stability in human liver microsomes[1].
TLR7 agonist 1 (10 μM) shows no CYP inhibition up to 10 μM in human liver microsomes[1].

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

Parmacokinetics
Species Dose Route Tmax Cmax AUC0-last
Rat[1] 5 mg/kg p.o. 1 h 142 ng/mL 365 ng·h/mL
In Vivo

TLR7 agonist 1 (compound 48) (5 mg/kg; p.o.; single dose) induces a peak plasma mIFN-α level of 2800 pg/mL at 4 hours in healthy C57BL/6 mice, with higher liver exposure than systemic exposure[1].

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

Molecular Weight

363.46

Formula

C21H25N5O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=NC2=C(C(C(N[C@@H](C)C3=CC=CC=C3)=O)=CC=C2)C(NCCCC)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (275.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7513 mL 13.7567 mL 27.5133 mL
5 mM 0.5503 mL 2.7513 mL 5.5027 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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. 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 2.7513 mL 13.7567 mL 27.5133 mL 68.7834 mL
5 mM 0.5503 mL 2.7513 mL 5.5027 mL 13.7567 mL
10 mM 0.2751 mL 1.3757 mL 2.7513 mL 6.8783 mL
15 mM 0.1834 mL 0.9171 mL 1.8342 mL 4.5856 mL
20 mM 0.1376 mL 0.6878 mL 1.3757 mL 3.4392 mL
25 mM 0.1101 mL 0.5503 mL 1.1005 mL 2.7513 mL
30 mM 0.0917 mL 0.4586 mL 0.9171 mL 2.2928 mL
40 mM 0.0688 mL 0.3439 mL 0.6878 mL 1.7196 mL
50 mM 0.0550 mL 0.2751 mL 0.5503 mL 1.3757 mL
60 mM 0.0459 mL 0.2293 mL 0.4586 mL 1.1464 mL
80 mM 0.0344 mL 0.1720 mL 0.3439 mL 0.8598 mL
100 mM 0.0275 mL 0.1376 mL 0.2751 mL 0.6878 mL
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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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Product Name:
TLR7 agonist 1
Cat. No.:
HY-111358
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