1. Immunology/Inflammation
  2. Toll-like Receptor (TLR) Interleukin Related IFNAR
  3. KBD4466

KBD4466 is an orally active potent TLR7 and TLR8 inhibitor with IC50s of 0.9 nM and 2.8 nM, respectively. KBD4466 inhibits the expression of inflammatory cytokines IL-6 and IFN-α. KBD4466 improves disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE). KBD4466 can be used in the study of autoimmune diseases.

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KBD4466

KBD4466 Chemical Structure

CAS No. : 3023713-87-0

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Description

KBD4466 is an orally active potent TLR7 and TLR8 inhibitor with IC50s of 0.9 nM and 2.8 nM, respectively. KBD4466 inhibits the expression of inflammatory cytokines IL-6 and IFN-α. KBD4466 improves disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE). KBD4466 can be used in the study of autoimmune diseases[1].

IC50 & Target[1]

TLR7

0.9 nM (IC50)

TLR8

2.8 nM (IC50)

IL-6

 

In Vitro

KBD4466 (Compound 19) inhibits TLR7 and TLR8 activity[1].

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

In Vivo

KBD4466 (Compound 19) (1 mg/kg, p.o., once) inhibits the production of IL-6 and IFN-α in R848 (HY-13740 )-challenged mouse model[1].

KBD4466 (10 mg/kg, p.o., once a day, 14 weeks) improves disease symptoms in the BXSB/MpJ mouse lupus model[1].

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

Animal Model: R848 (25 μg per mouse, i.p., 1 h, 4 h, 8 h, 16 h, 24 h after administration of compound 19)-challenged mouse (female C57BL/6 mice, 6-8 weeks old) model [1]
Dosage: 1 mg/kg
Administration: p.o., once
Result: Inhibited the production of IL-6, with an inhibition rate of 99.4% at 1 hour, more than 50% at 16 hours, and more than 90% at 8 hours.
Inhibited the production of IFN-α, with an inhibition rate of 98% at 16 h, 69% at 24 h.
Animal Model: SLE model using BXSB/MpJ transgenic mice (female BXSB/MpJ mice, 7 weeks).[1]
Dosage: 10 mg/kg
Administration: p.o., once a day, 14 weeks
Result: Improved survival rates ,the survival rate reached 100%.
Relieved splenomegaly and lymphadenopathy, and reduced plasma levels of autoantibodies, including anti-histone antibodies, anti-ribosomal P (anti-RiboP), and anti-double-stranded DNA (anti-dsDNA).
Reduced urine microalbumin (MALB), urine microalbumin to creatinine ratio (MALB/CREA), and urine total protein (UTP) levels.
Improved kidney swelling.
Molecular Weight

468.47

Formula

C24H23F3N6O

CAS No.
SMILES

CN1CCC(C2=NN=C([C@]34CN(C[C@]3(C4)C(F)(F)F)C5=C6C=CC=NC6=C(C=C5)C#N)O2)CC1

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
References
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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:
KBD4466
Cat. No.:
HY-176553
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