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Cat. No.: HY-181884

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TLR9-IN-3

TLR9-IN-3 is a TLR9 antagonist with an IC₅₀ of 0.4 μM. TLR9-IN-3 shows selectivity for TLR4 and TLR8, and inhibits CD69 activation in human whole blood with a corresponding IC₅₀ of 1.1 μM. TLR9-IN-3 can be used in research related to pulmonary fibrosis.

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

CAS No.: 2903190-66-7
Formula: C₁₈H₂₈N₈
Molecular Weight:356.47

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

TLR9-IN-3 Chemical Structure

CAS No.: 2903190-66-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

In Vitro

TLR9-IN-3 (Compound 20) has high metabolic stability in human and mouse liver microsomes (half-life > 120 min) but low stability in rat liver microsomes (half-life 3 min), and exhibits favorable passive permeability in PAMPA and Caco-2 assays^[1].
TLR9-IN-3 (0-25 μM) shows no cytotoxicity in A549, RAMOS, and THP-1 cell lines at concentrations up to 25 μM^[1].

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

In Vivo

TLR9-IN-3 (compound 20) (1-10 mg/kg; p.o.; QD; 2 days) exhibits statistically significant inhibition of pro-inflammatory and fibrogenic markers in a Bleomycin (HY-108345)-induced mouse lung injury model, with confirmed target engagement at 10 mg/kg^[1].

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

Animal Model:

C57BL/6 (male)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; QD; 2 days
Result:

Confirmed statistically significant target engagement via terminal blood CD69 detection at 10 mg/kg compared to the bleomycin control group.
Reduced bronchoalveolar lavage fluid (BALF) IL-6, TIMP-1, and soluble collagen levels in a statistically significant manner at 1 mg/kg, 3 mg/kg, and 10 mg/kg compared to the bleomycin control group.

Chemical Information

CAS No. 2903190-66-7
Molecular Weight 356.47
Formula C₁₈H₂₈N₈
SMILES

CN1CCN(C2=NC(NCCN(C)C)=NC(NC3=CC=CC=C3)=N2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mandler MD, et al. Discovery of Triazine-Based Toll-Like Receptor 9 Antagonists with Oral Activity. ACS Med Chem Lett. 2026;17(3):727-732. Published 2026 Feb 27. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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