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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- CAS No.: 3023713-87-0
- Formule: C24H23F3N6O
- Masse moléculaire:468.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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TLR7 0.9 nM (IC50) |
TLR8 2.8 nM (IC50) |
IL-6 |
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | F |
|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 3.6 h | 1297 ng/mL | 6247 ng·h/mL | 58 % |
| Rat | 5 mg/kg | p.o. | 5.1 h | 948 ng/mL | 7628 ng·h/mL | ＞99 % |
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.
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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]
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Dosage:1 mg/kg
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Administration:p.o., once
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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.
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Animal Model:SLE model using BXSB/MpJ transgenic mice (female BXSB/MpJ mice, 7 weeks).[1]
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Dosage:10 mg/kg
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Administration:p.o., once a day, 14 weeks
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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.
Chemical Information
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CAS No. 3023713-87-0
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Masse moléculaire 468.47
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Formule C24H23F3N6O
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KBD4466 Related Classifications
HY-176553 Related Classifications
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