2. Immunology/Inflammation
  3. Toll-like Receptor (TLR) Interleukin Related
  4. TLR7 antagonist-1

TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis.

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TLR7 antagonist-1

TLR7 antagonist-1 Chemical Structure

CAS No. : 3104353-70-7

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TLR7 antagonist-1 Related Antibodies

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Description

TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis[1].

IC50 & Target[1]

IL-1β

 

IL-6

 

TLR7

0.3 nM (IC50)

In Vitro

TLR7 antagonist-1 potently and selectively inhibits TLR7 in HEK-Blue-HTLR7 cells with an IC50 of 0.3 nM, while exhibiting much weaker activity against TLR8 and TLR9[1].
TLR7 antagonist-1 (0.005-5 μM; 12 h) inhibits TLR7-mediated inflammatory cytokines in a concentration-dependent manner in RAW264.7 and HEK-Blue-HTLR7 cells[1].

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

TLR7 antagonist-1 Related Antibodies

Real Time qPCR[1]

Cell Line: RAW264.7 cells, HEK-Blue-HTLR7 cells
Concentration: 0.005-5 μM (RAW264.7 cells); 0.005-5 μM (HEK-Blue-HTLR7 cells)
Incubation Time: 12 h
Result: Concentration-dependently downregulated R848-induced mRNA levels of IL-1β, IL-6, TNF-α in RAW264.7 cells.
Concentration-dependently reduced IFN-α mRNA levels in HEK-Blue-HTLR7 cells, with 0.5 μM showing better efficacy than 5 μM Enpatoran (HY-134581).
Parmacokinetics
Species Dose Route Cmax AUC0-t AUC0-∞ MRT0-∞ T1/2 Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 144.67 ng/mL 492.47 ng·h/mL 687.31 ng·h/mL 17.84 h 13.34 h / /
Rat[1] 10 mg/kg p.o. 153.25 ng/mL 2300.94 ng·h/mL 3329.35 ng·h/mL 20.76 h 13.63 h 6 h 46.66 %
In Vivo

TLR7 antagonist-1 (15-45 mg/kg; p.o.) effectively alleviates Imiquimod-induced psoriasis-like skin inflammation, systemic immune responses, and associated liver and renal dysfunction in female BALB/C mice, with dose-dependent reductions in inflammatory markers and tissue damage[1].

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

Animal Model: BALB/C (female, 6 weeks old, 15-16 g, imiquimod-induced psoriasis-like dermatitis)[1]
Dosage: 15 mg/kg; 45 mg/kg
Administration: p.o.
Result: Reduced PASI scores significantly compared to the model group, with only slight skin thickening appearing from day 18.
Reduced epidermis/stratum corneum thickening, Munro microabscesses, and subdermal lymphocyte infiltration compared to the model group, with dermis and cuticle thickness near control levels.
Reversed spleen enlargement, with spleen weights near control levels.
Reduced mRNA levels of NF-κB p65 and c-Rel in skin tissue in a dose-dependent manner, with high-dose group c-Rel levels comparable to control group.
Reduced serum and skin tissue levels of inflammatory cytokines IL-17A and IL-1β in a dose-dependent manner.
Normalized elevated white blood cell counts, lymphocyte counts, and lymphocyte percentages in the model group to control levels.
Reduced model group increases in ALT, AST, BUN, and Scr in a dose-dependent manner, with high-dose group showing the most significant liver and renal function protection.
Showed no significant differences in body weight, liver/kidney weight, or histopathological damage to liver, kidney, or spleen across groups.
Molecular Weight

455.90

Formula

C21H25ClF3N5O
CAS No.
SMILES

CC1=CN(C2=N1)C=C(C=C2OC)C3=CN=C(C(C(F)(F)F)=C3)N4CCC(C)(CC4)N.Cl
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
References
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TLR7 antagonist-1 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:

TLR7 antagonist-13104353-70-7Toll-like Receptor (TLR)Interleukin RelatedILTLR8IL-1βTLR7c-RelToll-like receptor 7MX1IL-6TNF-αNF-κB signaling pathwaysTLR9Inhibitorinhibitorinhibit

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