2. Disease Areas
  3. Respiratory Disease
  4. Pulmonary Disease
  5. Lung Fibrosis
  6. 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.

TLR9-IN-3

TLR9-IN-3 Chemical Structure

CAS No. : 2903190-66-7

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TLR9-IN-3 Related Antibodies

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Description

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[1].

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.

TLR9-IN-3 Related Antibodies
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.
Molecular Weight

356.47

Formula

C18H28N8
CAS No.
SMILES

CN1CCN(C2=NC(NCCN(C)C)=NC(NC3=CC=CC=C3)=N2)CC1
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Purity & Documentation
References
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TLR9-IN-3 Related Classifications

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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.

Keywords:

TLR9-IN-32903190-66-7human whole bloodrat liver microsomesmouse liver microsomesA549TLR4human liver microsomesTLR9CD69TLR8bleomycin-induced lung fibrosisInhibitorinhibitorinhibit

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